标签归档：hif

GEM-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GEM-5 

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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生物活性

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
体外研究
(In Vitro)

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner

体内研究
(In Vivo)

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.

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GEM-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GEM-5 

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
体外研究
(In Vitro)

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner

体内研究
(In Vivo)

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

HIF-2α-IN-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HIF-2α-IN-2  纯度: 98.01%

HIF-2α-IN-2 是一种低氧诱导因子(HIF-2α) 抑制剂，IC50 为16 nM，详细信息请参考专利文献 WO2015035223A1 中的化合物 232。

HIF-2α-IN-2

HIF-2α-IN-2 Chemical Structure

CAS No. : 1672666-82-8

规格 价格 是否有货 数量
5 mg ￥2800 In-stock
10 mg ￥3800 In-stock
50 mg ￥9900 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA)[1].

IC50 & Target

IC50: 16 nM (HIF-2α)[1]
分子量

365.35

Formula

C17H13F2NO4S
CAS 号

1672666-82-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (273.71 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7371 mL 13.6855 mL 27.3710 mL
5 mM 0.5474 mL 2.7371 mL 5.4742 mL
10 mM 0.2737 mL 1.3686 mL 2.7371 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Darryl David DIXON, et al. Aryl ethers and uses thereof. WO2015035223A1.

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LW6(Synonyms: HIF-1α inhibitor; LW8)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

LW6 (Synonyms: HIF-1α inhibitor; LW8) 纯度: 98.16%

LW6 (HIF-1α inhibitor) 是新颖的 HIF-1 抑制剂，IC50 值为 4.4 μM。LW6 降低 HIF-1α 蛋白表达，而不影响 HIF-1β 表达。

LW6(Synonyms: HIF-1α inhibitor; LW8)

LW6 Chemical Structure

CAS No. : 934593-90-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥726 In-stock
5 mg ￥660 In-stock
10 mg ￥990 In-stock
25 mg ￥2150 In-stock
50 mg ￥3850 In-stock
100 mg ￥6900 In-stock
200 mg   询价  
500 mg   询价  

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LW6 相关产品

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  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library

生物活性

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.

IC50 & Target

IC50: 4.4 μM (HIF-1)[1]
体外研究
(In Vitro)

LW6 affects the stability of the HIF-1α protein. LW6 promotes the degradation of wild type HIF-1α, but not of a DM-HIF-1α with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain. LW6 induces the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1α for proteasomal degradation. In the presence of LW6, knockdown of VHL does not abolish HIF-1α protein accumulation, indicating that LW6 degraded HIF-1α via regulation of VHL expression[2]. In MDCKII-BCRP cells overexpressing BCRP, LW6 enhances significantly the cellular accumulation of mitoxantrone, a BCRP substrate. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 µM[3]. LW6 inhibits the expression of HIF 1α induced by hypoxia in A549 cells at 20 µM, independently of the von Hippel Lindau protein. LW6 induces hypoxia selective apoptosis together with a reduction in the mitochondrial membrane potential[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In mice carrying xenografts of human colon cancer HCT116 cells, LW6 demonstrates strong anti-tumor efficacy in vivo and causes a decrease in HIF-1α expression in frozen-tissue immunohistochemical staining[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

435.51

Formula

C26H29NO5
CAS 号

934593-90-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (57.40 mM; Need ultrasonic)

DMF : 17.24 mg/mL (39.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2962 mL 11.4808 mL 22.9616 mL
5 mM 0.4592 mL 2.2962 mL 4.5923 mL
10 mM 0.2296 mL 1.1481 mL 2.2962 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.74 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.74 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Naik R, et al. Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors. J Med Chem. 2014 Nov 26;57(22):9522-38.

    [2]. Lee K, et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9.

    [3]. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein.

    [4]. Sato M, et al. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells. Mol Med Rep. 2015 Sep;12(3):3462-8.
Cell Assay
[2]

Inhibition of HIF-1a is assayed by a reporter assay using dualluciferase reporter assay system. HCT116 cells in 75-90% confluence are transiently co-transfected with pGL3-HRE-luciferase plasmid containing six copies of HREs from human VEGF genes and pRLSV40 encoding firefly renilla luciferase and incubated for 24 h. Cells are treated with LW6 or 17-AAG for 16 h before report assay. Luciferase activity is integrated over a 10 second period and measured using a luminometer[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: The mice receive the following treatments using a dosing vehicle solution, containing 10% dimethylacetamide, 10% Cremophor EL and 80% of sodium carbonate buffer (pH 10), by intraperitoneal (i.p.) injection: group1(control group; six mice), vehicle solution; group2 (six mice), LW6 at a dose of 10 and 20mg/kg (QD); and group 3 (six mice), topotecan at a dose of 2mg/kg, (Q2D), which is the dose and dosing schedule that showed more than 60% inhibition of growth of HCT116 tumors. The treatments are continued for 13 days[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Naik R, et al. Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors. J Med Chem. 2014 Nov 26;57(22):9522-38.

    [2]. Lee K, et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9.

    [3]. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein.

    [4]. Sato M, et al. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells. Mol Med Rep. 2015 Sep;12(3):3462-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Oltipraz(Synonyms: RP 35972; NSC 347901)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Oltipraz (Synonyms: RP 35972; NSC 347901) 纯度: 99.74%

Oltipraz 抑制 HIF-1α 激活, 这种作用具时间依赖性, 浓度 ≥ 10 μM 时完全消除 HIF-1α 诱导, Oltipraz 抑制 HIF-1α, IC50 为 10 μM。Oltipraz 还是一种强效的 Nrf2 激活剂。

Oltipraz(Synonyms: RP 35972; NSC 347901)

Oltipraz Chemical Structure

CAS No. : 64224-21-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
10 mg ￥500 In-stock
50 mg ￥900 In-stock
100 mg ￥1400 In-stock
200 mg ￥1800 In-stock
500 mg ￥2600 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

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  • Anti-Breast Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library

生物活性

Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.

IC50 & Target

IC50: 10 μM (HIF-1α)[1];
Nrf2[4]
体外研究
(In Vitro)

Oltipraz inhibits HIF-1α activity and HIF-1α-dependent tumor growth, which may result from a decrease in HIF-1α stability through S6K1 inhibition in combination with an H2O2-scavenging effect. Oltipraz treatment also inhibits HIF-1α activation stimulated by either hypoxia or CoCl2. Oltipraz is a cancer chemopreventive agent and has an inhibitory effect on angiogenesis and tumor growth. [1] Oltipraz is also a competitive inhibitor of this cytochrome P450, with an apparent Ki of 10 μM. [2]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In wild-type mice, hepatic levels of mRNA for all of the genes analyzed were significantly increased after Oltipraz treatment, with the highest increase (treated/control) for NQO1 mRNA levels (7.6-fold). The Northern blot analyses demonstrated that the observed increases in GST and NQO1 activities by Oltipraz in wild-type mice were preceded by significant elevations in RNA expression. Interestingly, mRNA levels of Nrf2 itself were increased more than 3-fold by Oltipraz treatment. [2]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

226.34

Formula

C8H6N2S3
CAS 号

64224-21-1
中文名称

吡噻硫酮；奥替普拉
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 6 mg/mL (26.51 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4181 mL 22.0907 mL 44.1813 mL
5 mM 0.8836 mL 4.4181 mL 8.8363 mL
10 mM 0.4418 mL 2.2091 mL 4.4181 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (4.42 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (4.42 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (4.42 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (4.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lee WH, et al. Oltipraz and dithiolethione congeners inhibit hypoxia-inducible factor-1alpha activity through p70 ribosomal S6 kinase-1 inhibition and H2O2-scavenging effect. Mol Cancer Ther. 2009 Oct;8(10):2791-802.

    [2]. Lv S, et al. Glucagon-induced extracellular cAMP regulates hepatic lipid metabolism. J Endocrinol. 2017 Aug;234(2):73-87.

    [3]. Ramos-Gomez M, et al. Sensitivity to carcinogenesis is increased and chemoprotective efficacy of enzyme inducers is lost in nrf2 transcription factor-deficient mice. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3410-5.

    [4]. Eba S, et al.The nuclear factor erythroid 2-related factor 2 activator oltipraz attenuates chronic hypoxia-induced cardiopulmonary alterations in mice.Am J Respir Cell Mol Biol. 2013 Aug;49(2):324-33.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

棘霉素HIF-1α抑制剂

发表于由

棘霉素HIF-1α抑制剂

高效，可逆的细胞渗透性HIF-1α抑制剂
≥98%

有货

棘霉素HIF-1α抑制剂

CAS编号 512-64-1 | 品牌：Jinpan
Echinomycin

MSDS

质检证书(CoA)

相似产品

  • 分子式 C51H64N12O12S2
  • 分子量1101.26

货号 (SKU) 包装规格 是否现货 价格 数量
E275307-1mg 1mg 期货 棘霉素HIF-1α抑制剂  
E275307-5mg 5mg 期货 棘霉素HIF-1α抑制剂  

基本信息

产品名称 棘霉素HIF-1α抑制剂
英文名称 Echinomycin
别名 N-[2,4,12,15,17,25-Hexamethyl-29-methylsulfanyl-3,6,10,13,16,19,23,26-octaoxo-11,24-di(propan-2-yl)-7-(quinoxaline-2-carbonylamino)-9,22-dioxa-28-thia-2,5,12,15,18,25-hexazabicyclo[12.12.3]nonacosan-20-yl]quinoxaline-2-carboxamide
英文别名 N-[2,4,12,15,17,25-Hexamethyl-29-methylsulfanyl-3,6,10,13,16,19,23,26-octaoxo-11,24-di(propan-2-yl)-7-(quinoxaline-2-carbonylamino)-9,22-dioxa-28-thia-2,5,12,15,18,25-hexazabicyclo[12.12.3]nonacosan-20-yl]quinoxaline-2-carboxamide
规格或纯度 ≥98%
运输条件 超低温冰袋运输
生化机理 强效，可逆的细胞渗透性HIF-1α抑制剂（EC 50 = 1.2 nM，低氧诱导的U215细胞中的HIF-1转录活性）。特异地插入DNA中。体内具有抗菌，抗病毒，抗血管生成和抗肿瘤作用。

一般描述

储存在-20℃。存放在干燥的条件下。该产品最多可存储12个月。

Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.

相关属性

CAS编号 512-64-1
溶解性 Soluble in DMSO to 5 mM
储存温度 -20°C储存,干燥
分子量 1101.26
分子式 C51H64N12O12S2
品牌 Jinpan
备注 如果有可能，您尽量在同一天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，这些产品最多可以使用一周。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
Smiles CC1C(=O)N(C2CSC(C(C(=O)N(C(C(=O)OCC(C(=O)N1)NC(=O)C3=NC4=CC=CC=C4N=C3)C(C)C)C)N(C(=O)C(NC(=O)C(COC(=O)C(N(C2=O)C)C(C)C)NC(=O)C5=NC6=CC=CC=C6N=C5)C)C)SC)C

GN44028

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GN44028  纯度: 99.37%

GN44028 是一种缺氧诱导因子(HIF)-1的有效抑制剂，其IC50 值为 14 nM。GN44028 能抑制低氧诱导的HIF-1α 的转录活性，但不抑制HIF-1α mRNA 的表达，HIF-1α 蛋白的累积或HIF-1α/HIF-1β 的异缘二聚化。

GN44028

GN44028 Chemical Structure

CAS No. : 1421448-26-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3190 In-stock
5 mg ￥2900 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

GN44028 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library

生物活性

GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization[1].

IC50 & Target

IC50: 14 nM (HIF-1)[1].
分子量

305.33

Formula

C18H15N3O2
CAS 号

1421448-26-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (163.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2751 mL 16.3757 mL 32.7515 mL
5 mM 0.6550 mL 3.2751 mL 6.5503 mL
10 mM 0.3275 mL 1.6376 mL 3.2751 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Minegishi H, et al. Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors. ACS Med Chem Lett. 2013 Jan 27;4(2):297-301.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

M1001

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

M1001  纯度: 99.77%

M1001 是一种较弱的 HIF-2α 激动剂，直接与 HIF-2α PAS-B 结构域结合，Kd 值为 667 nM。M1001 能够增强 HIF-2α-ARNT 复合体之间的稳定性。

M1001

M1001 Chemical Structure

CAS No. : 874590-32-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1320 In-stock
5 mg ￥1200 In-stock
10 mg ￥1950 In-stock
25 mg ￥3600 In-stock
50 mg ￥5760 In-stock
100 mg 询价

* Please select Quantity before adding items.

M1001 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library

生物活性

M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex[1].

IC50 & Target

Kd: 667 nM (HIF-2α)[1]
分子量

327.40

Formula

C17H17N3O2S
CAS 号

874590-32-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (763.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0544 mL 15.2718 mL 30.5437 mL
5 mM 0.6109 mL 3.0544 mL 6.1087 mL
10 mM 0.3054 mL 1.5272 mL 3.0544 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.33 mg/mL (7.12 mM); Clear solution

    此方案可获得 ≥ 2.33 mg/mL (7.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wu D, et al. Bidirectional modulation of HIF-2 activity through chemical ligands. Nat Chem Biol. 2019 Feb 25.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

小鼠缺氧诱导因子1α（HIF-1α）ELISA试剂盒BS-2779

发表于由

小鼠缺氧诱导因子1α（HIF-1α）ELISA试剂盒

  • 产品型号：BS-2779
  • 简要描述：小鼠缺氧诱导因子1α（HIF-1α）ELISA试剂盒金畔生物公司供应：ELISA试剂盒,荧光定量PCR耗材，移液器吸嘴，微量离心管，进口冻存管，细胞培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。
产品咨询在线客服
  • 产品简介

小鼠缺氧诱导因子1α(HIF-1α)ELISA试剂盒金畔生物公司供应：ELISA试剂盒,血清，荧光定量PCR耗材，移液器吸嘴，微量离心管，进口冻存管，细胞培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。

规格：96T/48T

BS-2779        小鼠缺氧诱导因子1α(HIF-1α)ELISA试剂盒

检测种属：人、大小鼠、豚鼠、兔子、猪、犬、牛羊、鸡鸭、猴ELISA试剂盒等种属。

保存条件及有效期：

1、试剂盒保存：2-8℃。

2、有效期：6个月

标记物：血清、血浆、组织匀浆等

【测试种属】犬、大小鼠、人、豚鼠、兔子、牛羊、猪、鸡鸭elisa试剂盒等种属
【储存方式】：2-8℃
【检测目的】用于测定血清，血浆及相关液体等样本。例如适合检测包括血清、血浆、尿液、胸腹水、灌洗液、脑脊液、细胞培养上清、组织匀浆等标本。
【用途】科研实验，不用于临床诊断。

小鼠缺氧诱导因子1α(HIF-1α)ELISA试剂盒

样本处理及要求：

1. 血清：室温血液自然凝固10-20分钟，离心20分钟左右(2000-3000转/分)。仔细收集上清，保存过程中如出现沉淀，应再次离心。

2. 血浆：应根据标本的要求选择EDTA或柠檬酸钠作为抗凝剂，混合10-20分钟后，离心20分钟左右(2000-3000转/分)。仔细收集上清，保存过程中如有沉淀形成，应该再次离心。

3. 尿液：用无菌管收集，离心20分钟左右(2000-3000转/分)。仔细收集上清，保存过程中如有沉淀形成，应再次离心。胸腹水、脑脊液参照实行。

4. 细胞培养上清：检测分泌性的成份时，用无菌管收集。离心20分钟左右(2000-3000转/分)。仔细收集上清。检测细胞内的成份时，用PBS(PH7.2-7.4)稀释细胞悬液，细胞浓度达到100万/ml左右。通过反复冻融，以使细胞破坏并放出细胞内成份。离心20分钟左右(2000-3000转/分)。仔细收集上清。保存过程中如有沉淀形成，应再次离心。

5. 组织标本：切割标本后，称取重量。加入一定量的PBS，PH7.4。用液氮迅速冷冻保存备用。标本融化后仍然保持2-8℃的温度。加入一定量的PBS(PH7.4)，用手工或匀浆器将标本匀浆充分。离心20分钟左右(2000-3000转/分)。仔细收集上清。分装后一份待检测，其余冷冻备用。

6. 标本采集后尽早进行提取，提取按相关文献进行，提取后应尽快进行实验。若不能马上进行试验，可将标本放于-20℃保存，但应避免反复冻融.

7. 不能检测含NaN3的样品，因NaN3抑制辣根过氧化物酶的(HRP)活性。

小鼠缺氧诱导因子1α(HIF-1α)ELISA检测试剂盒操作步骤：

小鼠缺氧诱导因子1α（HIF-1α）ELISA试剂盒BS-2779

检测试剂盒组成：
试剂盒组成48 孔配置96 孔配置保存
说明书1 份1 份
封板膜2 片(48)2 片(96)
密封袋1 个1 个
酶标包被板1×481×962-8℃保存
标准品：540μg/L0.5ml×1 瓶0.5ml×1 瓶2-8℃保存
标准品稀释液1.5ml×1 瓶1.5ml×1 瓶2-8℃保存
酶标试剂3 ml×1 瓶6 ml×1 瓶2-8℃保存
样品稀释液3 ml×1 瓶6 ml×1 瓶2-8℃保存
显色剂 A 液3 ml×1 瓶6 ml×1 瓶2-8℃保存
显色剂 B 液3 ml×1 瓶6 ml×1 瓶2-8℃保存
终止液3 ml×1 瓶6 ml×1 瓶2-8℃保存
浓缩洗涤液(20ml×20 倍)×1 瓶(20ml×30 倍)×1 瓶2-8℃保存

可重复用的瓶顶过滤器，聚砜;硅胶O形环;聚丙烯真空接头，适合瓶颈尺寸为45mm的玻璃培养基瓶，上室容量500ml

QSP吸头加长带滤芯吸头/滤芯无菌吸头

带滤芯吸头/移液器吸嘴

吸头/带滤芯超微吸头

Oak Ridge 离心管,聚碳酸酯;聚丙烯螺旋盖

滤芯吸头加长带刻度盒装96/盒

QSP吸头无酶无热源滤芯吸头1000ul现货

Nunc U96 透明微孔板 F96氨基酶标板

带滤芯吸头|通用型移液器吸嘴

QSP带滤芯加长进口吸头

Nunc -20℃Labtop便携式冰盒

Nunc MAX-100 CryostoreTM冻存管盒，Megamax-100冻存管盒，带10*10间隔器

易认安全洗瓶，LDPE，白色LDPE或PPCO瓶体;PP或HDPE盖;PPCO填充管，500ml容量，甲醇，绿色瓶盖

颜色标记的UnitaryTM 分类洗瓶，低密度聚乙烯瓶体;聚丙烯螺旋盖

广口洗瓶，低密度聚乙烯瓶体;聚丙烯螺旋盖/杆;聚丙烯共聚物吸管，500ml容量

 

产品用途：可用于科研实验,不用于临床治疗！

大鼠低氧诱导因子1α（HIF-1α）ELISA试剂盒BS-3266

发表于由

大鼠低氧诱导因子1α（HIF-1α）ELISA试剂盒

  • 产品型号：BS-3266
  • 简要描述：大鼠低氧诱导因子1α（HIF-1α）ELISA试剂盒上海金畔生物供应ELISA试剂盒种属全，实验室耗材种类全，PCR耗材，离心管，进口吸头等等。
产品咨询在线客服
  • 产品简介

大鼠低氧诱导因子1α(HIF-1α)ELISA试剂盒金畔生物公司供应：ELISA试剂盒，血清，荧光定量PCR耗材，移液器吸嘴，微量离心管，进口冻存管，细胞培养皿，培养板，培养瓶，吸头，仪器及手套，色谱耗材，针头过滤器。

大鼠ELISA试剂盒  大鼠ELISAkit   试剂盒代测

英文名：HIF-1α  ELISAkit

产品货号        产品名称                          

BS-3266 大鼠低氧诱导因子1α(HIF-1α)ELISA检测试剂盒

产品规格：96T/48T

品牌:金畔

种属:大鼠

检测波长:450 nm

所需样本体积: 50-100ul

适用范围:仅供科研

保存及有效期:2-8℃，六个月

检测目的:用于测定血清，血浆及相关液体等样本。例如适合检测包括血清、血浆、尿液、胸腹水、灌洗液、脑脊液、细胞培养上清、组织匀浆等标本。

金畔供应的种属有：人、大鼠、小鼠、豚鼠、兔子、猪犬、牛羊、鸡鸭、植物ELISA试剂盒等

大鼠低氧诱导因子1α(HIF-1α)ELISA试剂盒

【*优势】

1、产品种类齐全、质量可靠、*、灵敏度高、效果稳定、易保存、操作简便

2、免费提供产品报价、实验原理、产品用途及中英文说明书

三.金畔ELISA试剂盒组成：产品组成48孔配置96孔配置Storage

标准品：180ng/L0.5ml×1瓶0.5ml×1瓶2-8℃

标准品稀释液1.5ml×1瓶1.5ml×1瓶2-8℃

酶标试剂3ml×1瓶6ml×1瓶2-8℃

样品稀释液3ml×1瓶6ml×1瓶2-8℃

显色剂A液3ml×1瓶6ml×1瓶2-8℃

显色剂B液3ml×1瓶6ml×1瓶2-8℃

终止液3ml×1瓶6ml×1瓶2-8℃

浓缩洗涤液(20ml×20倍)×1瓶(20ml×30倍)×1瓶2-8℃

酶标包被板1×481×962-8℃

封板膜2片2片RT

密封袋1个1个RT

说明书1份1份RT

大鼠低氧诱导因子1α(HIF-1α)ELISA检测试剂盒

四.操作步骤：

大鼠低氧诱导因子1α（HIF-1α）ELISA试剂盒BS-3266

 

五.注意事项：

1.试剂盒从冷藏环境中取出应在室温平衡15-30分钟后方可使用，酶标包被板开封后如未用完，板条应装入密封袋中保存。

2.浓洗涤液可能会有结晶析出，稀释时可在水浴中加温助溶，洗涤时不影响结果。

3.各步加样均应使用加样器，并经常校对其准确性，以避免试验误差。一次加样时间控制在5分钟内，如标本数量多，推荐使用排枪加样。

4.请每次测定的同时做标准曲线，做复孔。如标本中待测物质含量过高(样本OD值大于标准品孔孔的OD值)，请先用样品稀释液稀释一定倍数(n倍)后再测定，计算时请乘以总稀释倍数(×n×5)。

5.封板膜只限一次性使用，以避免交叉污染。

6.底物请避光保存。

7.严格按照说明书的操作进行，试验结果判定必须以酶标仪读数为准.

8.所有样品，洗涤液和各种废弃物都应按传染物处理。

9.本试剂不同批号组分不得混用。

10.如与英文说明书有异，以英文说明书为准。

六.标准曲线的绘制方法：

可以采用各种绘图软件来绘制ELISA标准曲线，我公司以“Curve Exert1.3”软件为例，绘制的ELISA标准曲线如下：

大鼠低氧诱导因子1α（HIF-1α）ELISA试剂盒BS-3266

大鼠低氧诱导因子1α(HIF-1α)ELISA检测试剂盒

计算：以标准物的浓度为横坐标，OD值为纵坐标，在坐标纸上绘出标准曲线，根据样品的OD值由标准曲线查出相应的浓度;再乘以稀释倍数;或用标准物的浓度与OD值计算出标准曲线的直线回归方程式，将样品的OD值代入方程式，计算出样品浓度，再乘以稀释倍数，即为样品的实际浓度。

进口PCR耗材八联排,PCR单管

0.2ml透明8联排PCR管凸盖,非灭菌

100μl 96孔PCR板 白色/乳白色

0.2ml荧光定量8联排PCR管(平盖)

进口耗材0.1ml8联排实时荧光定量PCR管平盖

40μl 384孔黑色全裙边PCR 板

100μl 96孔白色无裙边PCR板

100μl 96孔白色半裙边PCR板

0.1ml 白色8联排实时荧光定量PCR管平盖

0.2ml 8联排实时荧光定量PCR管盖, 平盖, 无DNA酶无RNA酶无热源, 无色

0.2ml 8联排实时荧光定量PCR管, 超薄壁 无DNA酶无RNA酶无热源, 无色

0.2ml 8联排管盖, 拱顶盖(凸盖), 无DNA酶无RNA酶无热源, 无色

3ML塑料刻度巴氏吸管,滴量52ul,长178mm,单支灭菌包装

3ML塑料刻度巴氏吸管,滴量48ul,长160mm,单支灭菌包装

3ML塑料刻度巴氏吸管,滴量52ul,长162mm,单支灭菌包装

elisa试剂盒是一种敏感性高、特异性强、重复性好的实验诊断方法，由于其试剂稳定、易保存、操作简便、结果判断较客观等因素，以及既适宜于大规模筛查试验又可以用于少量标本的检测，既可以做定性试验也可以做定量分析等优点，已广泛应用于微生物学、寄生虫学、肿瘤学和细胞因子等领域。

 

产品用途：可用于科研实验,不用于临床治疗！

FM19G11

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FM19G11 

FM19G11 是一种 hypoxia-inducible factor-1-alpha (HIF-1α) 抑制剂，在 HeLa 细胞中抑制缺氧诱导的荧光素酶活性，其 IC50 值为 80 nM。当 HIF-1α 途径在常氧条件下失活时，FM19G11 会调节其他信号途径，包括 mTOR 和 PI3K/Akt/eNOS。

FM19G11

FM19G11 Chemical Structure

CAS No. : 329932-55-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions[1][2].

IC50 & Target

HIF-1α[1]
体外研究
(In Vitro)

FM19G11 (30-300 nM) inhibits HIFα proteins in the HeLa cell lines[1].
FM19G11 (500 nM) promotes oligodendrocyte differentiation under hypoxia[1].
FM19G11 (300 nM; 3 days) suppresses the mRNA levels of O6-methylguanine DNA-methyltransferase (MGMT) significantly in hypoxic GBM‐XD, hypoxic T98G, and normoxic T98G cells[2].
M19G11 (300 nM; 3 days) significantly enhances the pro‐apoptotic effect of temozolomide (TMZ), although FM19G11 does not induce apoptosis by itself[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: GBM‐XD and T98G cells
Concentration: 300 nM
Incubation Time: 3 days
Result: Had no cytotoxicity by itself.
Enhanced the cytotoxicity of TMZ in hypoxic GBM-XD cells, hypoxic T98G cells, and normoxic T98G cells.

Western Blot Analysis[2]

Cell Line: GBM‐XD and T98G cells
Concentration: 300 nM
Incubation Time: 3 days
Result: Suppressed MGMT expression significantly in both cell lines in hypoxic culture.
Downregulated MGMT expression substantially inT98G cells in normoxic culture.

体内研究
(In Vivo)

FM19G11 ( intramedullary injection; 1-8 weeks) improves locomotion in severe spinal cord injury (SCI)[3].
FM19G11 ( intramedullary injection; 8 weeks) induces the expression of GAP43, an axon growth marker, and RIP, a marker for myelinated oligodendrocytes at the injury[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

463.40

Formula

C23H17N3O8
CAS 号

329932-55-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Victoria MM, et, al. FM19G11, a new hypoxia-inducible factor (HIF) modulator, affects stem cell differentiation status. J Biol Chem. 2010 Jan 8; 285(2): 1333-42.

    [2]. You CG, et, al. FM19G11 inhibits O 6 -methylguanine DNA-methyltransferase expression under both hypoxic and normoxic conditions. Cancer Med. 2018 May 15; 7(7): 3292-3300.

    [3]. Ana AA, et, al. FM19G11 and Ependymal Progenitor/Stem Cell Combinatory Treatment Enhances Neuronal Preservation and Oligodendrogenesis after Severe Spinal Cord Injury. Int J Mol Sci. 2018 Jan 9; 19(1): 200.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PT2399

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PT2399  纯度: 99.83%

PT2399 是一种高效、选择性的 HIF-2α 的拮抗剂，能直接结合 HIF-2α PAS B 结构域，IC50 值为 6 nM。PT2399 具有高效的体内抗肿瘤活性。

PT2399

PT2399 Chemical Structure

CAS No. : 1672662-14-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4070 In-stock
5 mg ￥3700 In-stock
10 mg ￥6200 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

PT2399 相关产品

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生物活性

PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo[1][2][3].

IC50 & Target

IC50: 6 nM (HIF-2α)[3]
体外研究
(In Vitro)

PT2399 (compound 10f) inhibits HIF-2α with an IC50 of 6 nM[3].
PT2399 can bind directly to the HIF-2α PAS B domain, and cripple HIF-2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT)[2].
PT2399 (20 μM) causes off-target toxicity because it inhibits the proliferation of HIF-2α −/− 786-O cells and other cancer cell lines with undetectable HIF-2α[2].
PT2399 (0.2–2 μM; 0-21 days) inhibits 786-O cells soft agar growth[2].
PT2399 represses various HIF target genes in 786-O VHL−/− ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: 786-O cells
Concentration: 0 μM, 0.2 μM, 2 μM
Incubation Time: 0-21 days
Result: Inhibited 786-O cell soft agar growth at 0.2–2 μM.

体内研究
(In Vivo)

PT2399 inhibits tumor cell proliferation 3.5 fold in renal cell carcinoma (RCC) bearing mice[1].
PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice[1].
PT2399 (100 mg/kg; oral gavage; every 12 hours) is more active than SU 11248, and inhibits tumor growth in several SU 11248-resistant tumors in RCC bearing mice [1].
PT2399 directly inhibits HIF-2α causes tumor regression in preclinical models of primary and metastatic pVHL-defective ccRCC in an on-target fashion[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice with RCC tumorgraft[1]
Dosage: 100 mg/kg
Administration: Oral gavage; every 12 hours
Result: More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.

分子量

419.32

Formula

C17H10F5NO4S
CAS 号

1672662-14-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : ≥ 200 mg/mL (476.96 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3848 mL 11.9241 mL 23.8481 mL
5 mM 0.4770 mL 2.3848 mL 4.7696 mL
10 mM 0.2385 mL 1.1924 mL 2.3848 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.98 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.98 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.98 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.98 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.98 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117.

    [2]. Cho H, et al. On-Target Efficacy of a HIF2α Antagonist in Preclinical Kidney Cancer Models. Nature. Nature. 2016 Nov 3;539(7627):107-111.

    [3]. Wehn PM, et al. Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J Med Chem. 2018 Nov 8;61(21):9691-9721.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Izilendustat hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Izilendustat hydrochloride 

Izilendustat (hydrochloride) 是一种有效的脯氨酰羟化酶 (prolyl hydroxylase) 抑制剂，可稳定缺氧诱导因子-1 α (HIF-1α) 和缺氧诱导因子-2 (HIF-2)。Izilendustat (hydrochloride) 具有研究 HIF-1α 相关疾病的潜力，包括外周血管疾病（PVD）、冠状动脉疾病（CAD）、心力衰竭、缺血、贫血、结肠炎和其他炎症性肠病 (信息提取自专利 WO2011057115A1/WO2011057112A1/WO2011057121A1)。

Izilendustat hydrochloride

Izilendustat hydrochloride Chemical Structure

CAS No. : 1303513-80-5

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Izilendustat hydrochloride 的其他形式现货产品:

Izilendustat

生物活性

Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1)[1][2][3].

IC50 & Target

prolyl hydroxylase[1]
分子量

470.39

Formula

C22H29Cl2N3O4
CAS 号

1303513-80-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Joseph H, et al. Prolyl hydroxylase inhibitors. Patent WO2011057115A1.

    [2]. Robert Shalwitz, et al. Methods for increasing the stabilization of hypoxia inducible factor-1 alpha. Patent WO2011057112A1.

    [3]. Joseph H, et al. Compositions and methods for treating colitis. Patent WO2011057121A1.

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Deoxyshikonin

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Deoxyshikonin  纯度: 99.96%

Deoxyshikonin 从紫草 Lithospermum erythrorhizon 中分离，具有抗肿瘤活性。Deoxyshikonin增加 HMVEC-dLy 中 VEGF-C 和 VEGF-A mRNA 的表达，促进 HIF-1α 和 HIF-1β 亚基相互作用，并与 HIF 特异性 DNA 序列结合。Deoxyshikonin 在体外具有促血管生成作用。Deoxyshikonin 显示出显着的协同抗微生物活性, S. pneumonia (MIC =17μg/mL)，也显示出对 MRSA 的显着抑制活性。

Deoxyshikonin

Deoxyshikonin Chemical Structure

CAS No. : 43043-74-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2696 In-stock
5 mg ￥2550 In-stock
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Deoxyshikonin 相关产品

•相关化合物库:

  • Natural Product Library Plus
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生物活性

Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro[1]. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA[2].

分子量

272.30

Formula

C16H16O4
CAS 号

43043-74-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (122.40 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6724 mL 18.3621 mL 36.7242 mL
5 mM 0.7345 mL 3.6724 mL 7.3448 mL
10 mM 0.3672 mL 1.8362 mL 3.6724 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.18 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Prangsaengtong O, et al. Enhancement of Lymphangiogenesis In Vitro via the Regulations of HIF-1α Expression and Nuclear Translocation by Deoxyshikonin. Evid Based Complement Alternat Med. 2013;2013:148297.

    [2]. Zhang S, et al. Antibacterial effects of Traditional Chinese Medicine monomers against Streptococcus pneumoniae via inhibiting pneumococcal histidine kinase (VicK). Front Microbiol. 2015 May 20;6:479.

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Verucopeptin

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Verucopeptin  纯度: 98.42%

Verucopeptin 是一种有效的 HIF-1 (IC50=0.22 μM) 抑制剂，可以降低 HIF-1 靶基因的表达和 HIF-1α 的蛋白水平。通过直接靶向 v-ATPase ATP6V1G 亚基 (但不靶向 ATP1V1B2 或 ATP6V1D)，Verucopeptin 强烈抑制 v-ATPase 活性。Verucopeptin 对耐药性癌细胞表现出抗肿瘤活性，常用作癌症相关研究。

Verucopeptin

Verucopeptin Chemical Structure

CAS No. : 138067-14-8

规格 价格 是否有货 数量
50 μg ￥2500 In-stock

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生物活性

Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels[1][2]. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research[3].

IC50 & Target

IC50: 0.22 μM (HIF-1)[2]
IC50: v-ATPase ATP6V1G subunit[3]
体外研究
(In Vitro)

ATP6V1G, a subunit of the vacuolar H+-ATPase (v-ATPase)[3].
Verucopeptin (0-30 μM; 72 h) shows excellent antitumor activity against K562R cells, with an IC50 of 388 nM, although these cells exhibit resistance to some other chemotherapeutic agents, such as Taxol and vincristine at concentrations of 10 μM[3].
Verucopeptin (0-1 μM) shows broad antiproliferative activity, with IC50 values of less than 100 nM against 66% of the cell lines evaluated among a total of 1,094 cancer cell lines. Moreover,Verucopeptin displays tissue specificity, such as leukemia, lymphoma, and melanoma, are classified in the lower IC50 groups, while the higher IC50 groups including other cancer types, such as non-small cell lung cancer[3].
Verucopeptin (10 nM; 1 hour) pretreatment blocks VE-P labeling of ATP6V1G1 but not ATP1V1B2 or ATP6V1D in a competitive binding assay. Verucopeptin shows substantial inhibition of v-ATPase activity and suppresses lysosomal acidification in vitro, as does Baf A1, although to a lesser extent[3].
Verucopeptin (0-500 nM; 1 hour) exhibits substantial inhibition of p-S6K as well as p-4EBP1 at concentrations of 10-200 nM. Additionally, Verucopeptin attenuates the phosphorylation of most of the tested mTORC1 downstream substrates, including p-4EBP1, pmTORS2448, p-mTORS2481, p-Rictor, p-ULK1, and p-Grb10, at concentrations ranging from 50 nM to 500 nM[3].
Verucopeptin (0-335 nM; 24 hour) decreases the HIF-1 protein level in a dose-dependent manner but has no effects on c-Raf in HT1080 cells. However, the known hsp90 inhibitor Tanespimycin (HY-10211) inhibits both HIF-1 and c-Raf expression in cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Verucopeptin (intravenous injection; 1 mg/kg; twice daily; 7 days) substantially represses tumor growth without significant body weight loss or gross signs of toxicity. HE staining indicated that Verucopeptin potently induces cell death and abrogates mTORC1 signaling by dephosphorylation of S6K and 4EBP1[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice by subcutaneous injection of SGC7901/VCR cells[3]
Dosage: 1 mg/kg
Administration: Intravenous injection; 1 mg/kg; twice daily; 7 days
Result: Exhibited profound antitumor efficacy in vivo against MDR tumors.

分子量

896.08

Formula

C43H73N7O13
CAS 号

138067-14-8
Sequence Shortening

L-{Aaa}-G-{Sar}-G-{Sar} Lactone:(Leu1-Sar6)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Aya Yoshimura, et al.Structure Elucidation of Verucopeptin, a HIF-1 Inhibitory Polyketide-Hexapeptide Hybrid Metabolite from an Actinomycete. Org Lett. 2015 Nov 6;17(21):5364-7.

    [2]. Nobuaki Takahashi, et al. Total synthesis of verucopeptin, an inhibitor of hypoxia-inducible factor 1 (HIF-1). Chem Commun (Camb). 2019 Oct 1;55(79):11956-11959.

    [3]. Yuezhou Wang, et al. Pharmacological Targeting of Vacuolar H +-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Jun 30;S2451-9456(20)30234-8.

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HIF-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HIF-IN-1 

HIF-IN-1 (Compound 3c) 是一种缺氧诱导因子 (HIF-1) 抑制剂。HIF-IN-1 抑制 HIF-1α 蛋白聚集，不影响 HIF-1α mRNA 的水平。HIF-IN-1 无明显细胞毒性。

HIF-IN-1

HIF-IN-1 Chemical Structure

CAS No. : 2393928-76-0

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生物活性

HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity[1].

分子量

260.29

Formula

C17H12N2O
CAS 号

2393928-76-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Fuse S, et al. Design, synthesis, and evaluation of indeno[2,1-c]pyrazolones for use as inhibitors against hypoxia-inducible factor (HIF)-1 transcriptional activity. Bioorg Med Chem. 2020 Jan 1;28(1):115207.

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GEM-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GEM-5 

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
体外研究
(In Vitro)

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner

体内研究
(In Vivo)

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.

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