标签归档：hsp

HDAC/HSP90-IN-4

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HDAC/HSP90-IN-4 

这些化合物具有强大的HDAC 和HSP90 抑制活性，化合物20（HDAC IC50 = 194 nM; HSP90α IC50 = 153 nM）和化合物26（(HDAC IC50= 360 nM; HSP90α IC50 = 77 nM)表现出最强的HDAC和HSP90α抑制活性。这两种化合物都能诱导HSP90 表达并下调HSP90 客户蛋白，而HSP90 客户蛋白在调节癌细胞的生存和侵袭中起着重要作用。

HDAC/HSP90-IN-4

HDAC/HSP90-IN-4 Chemical Structure

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生物活性

These compounds have strong hdac and hsp90 inhibitory activities. Compound 20 (HDAC ic50   =   194   nm; Hsp90 α < b> Ic50 =   153   nm) and compound 26 ((HDAC ic50=   360   nm; Hsp90 α < b> Ic50   =   77   nm) shows the strongest HDAC and HSP90 α Inhibitory activity. Both compounds can induce hsp90 expression and down regulate hsp90 client proteins, which play an important role in regulating the survival and invasion of cancer cells.

Formula

C20H23N3O6
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]. Mehndiratta S,et al. N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. Eur J Med Chem. 2020 Jan 1;185:111725.

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HDAC6/HSP90-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。

HDAC6/HSP90-IN-1 

HDAC6/HSP90-IN-1 (化合物17) 是一种有效的选择性的 HDAC6 和 HSP90 的双重抑制剂，IC50 值分别为 4.3 和 46.8 nM。HDAC6/HSP90-IN-1 可下调 INF-γ 处理的 H1975 肺癌细胞中 PD-L1 的表达。HDAC6/HSP90-IN-1 在 H1975 异种移植小鼠中抑制肿瘤生长。

HDAC6/HSP90-IN-1

HDAC6/HSP90-IN-1 Chemical Structure

CAS No. : 2411955-43-4

规格 是否有货
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生物活性

HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice[1].

IC50 & Target

HDAC6

4.32 nM (IC50)

HSP90

46.8 nM (IC50)

HDAC3

1312 nM (IC50)

HDAC1

1878 nM (IC50)

HDAC8

3720 nM (IC50)

分子量

511.61

Formula

C28H37N3O6
CAS 号

2411955-43-4
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]. Ojha R, et al. Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo. Eur J Med Chem. 2020 Mar 15;190:112086.

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HSP90-IN-10

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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。

HSP90-IN-10 

HSP90-IN-10 (Compound 16s) 是一种有效的 HSP90 抑制剂。 HSP90-IN-10 对 HCC1954 乳腺癌细胞具有很强的抗增殖能力，IC50 值为 6 µM。HSP90-IN-10 不抑制正常上皮细胞的生长。HSP90-IN-10 还诱导细胞凋亡 (apoptosis)。

HSP90-IN-10

HSP90-IN-10 Chemical Structure

规格 是否有货
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生物活性

HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis[1].

分子量

543.54

Formula

C30H26FN3O6
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]. Piven YA, et al. Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Bioorg Med Chem. 2022 Jan 1;53:116521.

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HSP90-IN-11

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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。

HSP90-IN-11 

HSP90-IN-11 (Compound 12c) 是一种有效的 HSP90 抑制剂。 HSP90-IN-11 显示出与 AUY-922 (Luminespib) 相当的有效 HSP90α 抑制作用。HSP90-IN-11 在 CRC 和 NSCLC 细胞中显示出显着的抗增殖活性，在两位数 nM 范围内。HSP90-IN-11 导致 NSCLC 细胞中客户蛋白 EGFR 和 Akt 的快速降解。HSP90-IN-11 诱导亚 G1 期群体的显着积累。

HSP90-IN-11

HSP90-IN-11 Chemical Structure

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生物活性

HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population[1].

分子量

511.54

Formula

C27H30FN3O6
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]. Wu WC, et al. Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells. Eur J Med Chem. 2020 Oct 1;203:112540.

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Apatorsen(Synonyms: OGX-427)

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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。

Apatorsen (Synonyms: OGX-427)

Apatorsen 是一种靶向Hsp27 mRNA的反义寡核苷酸，抑制Hsp27蛋白的产生。

Apatorsen(Synonyms: OGX-427)

Apatorsen Chemical Structure

规格 是否有货
1 mg 询价
5 mg 询价

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生物活性

Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.

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]. Spigel DR, Shipley DL, Waterhouse DM, et al. A Randomized, Double-Blinded, Phase II Trial of Carboplatin and Pemetrexed with or without Apatorsen (OGX-427) in Patients with Previously Untreated Stage IV Non-Squamous-Non-Small-Cell Lung Cancer: The SPRUCE Trial. Oncologist. 2019;24(12):e1409-e1416.

    [2]. Yu EY, Ellard SL, Hotte SJ, et al. A randomized phase 2 study of a HSP27 targeting antisense, apatorsen with prednisone versus prednisone alone, in patients with metastatic castration resistant prostate cancer. Invest New Drugs. 2018;36(2):278-287.

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Apatorsen(Synonyms: OGX-427)

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。

Apatorsen (Synonyms: OGX-427)

Apatorsen 是一种靶向Hsp27 mRNA的反义寡核苷酸，抑制Hsp27蛋白的产生。

Apatorsen(Synonyms: OGX-427)

Apatorsen Chemical Structure

规格 是否有货
1 mg 询价
5 mg 询价

* Please select Quantity before adding items.

生物活性

Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.

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]. Spigel DR, Shipley DL, Waterhouse DM, et al. A Randomized, Double-Blinded, Phase II Trial of Carboplatin and Pemetrexed with or without Apatorsen (OGX-427) in Patients with Previously Untreated Stage IV Non-Squamous-Non-Small-Cell Lung Cancer: The SPRUCE Trial. Oncologist. 2019;24(12):e1409-e1416.

    [2]. Yu EY, Ellard SL, Hotte SJ, et al. A randomized phase 2 study of a HSP27 targeting antisense, apatorsen with prednisone versus prednisone alone, in patients with metastatic castration resistant prostate cancer. Invest New Drugs. 2018;36(2):278-287.

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

Apatorsen(Synonyms: OGX-427)

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。

Apatorsen (Synonyms: OGX-427)

Apatorsen 是一种靶向Hsp27 mRNA的反义寡核苷酸，抑制Hsp27蛋白的产生。

Apatorsen(Synonyms: OGX-427)

Apatorsen Chemical Structure

规格 是否有货
1 mg 询价
5 mg 询价

* Please select Quantity before adding items.

生物活性

Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.

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]. Spigel DR, Shipley DL, Waterhouse DM, et al. A Randomized, Double-Blinded, Phase II Trial of Carboplatin and Pemetrexed with or without Apatorsen (OGX-427) in Patients with Previously Untreated Stage IV Non-Squamous-Non-Small-Cell Lung Cancer: The SPRUCE Trial. Oncologist. 2019;24(12):e1409-e1416.

    [2]. Yu EY, Ellard SL, Hotte SJ, et al. A randomized phase 2 study of a HSP27 targeting antisense, apatorsen with prednisone versus prednisone alone, in patients with metastatic castration resistant prostate cancer. Invest New Drugs. 2018;36(2):278-287.

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

HSP70-IN-3

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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。

HSP70-IN-3 

HSP70-IN-3 是一种有效的热休克蛋白 (HSP70) 抑制剂 (ASZ001 和 C3H10T1/2 的 IC50 分别为1.1和1.9 μM)。HSP70-IN-3 具有抗 Hedgehog 信号转导通路活性和抗增殖活性，并降低致癌转录因子 GLI1 的表达。

HSP70-IN-3

HSP70-IN-3 Chemical Structure

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

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生物活性

HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1[1].

IC50 & Target

IC50: 1.1 μM (HSP70) in ASZ001, 1.9 μM (HSP70) in C3H10T1/2[1]
体外研究
(In Vitro)

HSP70-IN-3 (compound 8) (5 μM; 72 hours) has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity in ASZ001 cells[1].
HSP70-IN-3 can almost completely abolish the expression of Gli1 mRNA in ASZ001 cells after 20-hour incubation[1].

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

Cell Proliferation Assay

Cell Line: ASZ001 cells[1]
Concentration: 5 μM
Incubation Time: 72 hours
Result: Showed anti-Hh(Hedgehog signaling) activity and anti-proliferative activity.

Cell Proliferation Assay

Cell Line: ASZ001 cells[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: After a 20-h incubation with HSP70-IN-3, expression of Gli1 mRNA was almost completely abolished.

分子量

883.23

Formula

C48H78N6O7S
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]. Wen J, et al. Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma. Eur J Med Chem. 2022;228:114005.

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HSP70-IN-3

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。

HSP70-IN-3 

HSP70-IN-3 是一种有效的热休克蛋白 (HSP70) 抑制剂 (ASZ001 和 C3H10T1/2 的 IC50 分别为1.1和1.9 μM)。HSP70-IN-3 具有抗 Hedgehog 信号转导通路活性和抗增殖活性，并降低致癌转录因子 GLI1 的表达。

HSP70-IN-3

HSP70-IN-3 Chemical Structure

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

HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1[1].

IC50 & Target

IC50: 1.1 μM (HSP70) in ASZ001, 1.9 μM (HSP70) in C3H10T1/2[1]
体外研究
(In Vitro)

HSP70-IN-3 (compound 8) (5 μM; 72 hours) has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity in ASZ001 cells[1].
HSP70-IN-3 can almost completely abolish the expression of Gli1 mRNA in ASZ001 cells after 20-hour incubation[1].

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

Cell Proliferation Assay

Cell Line: ASZ001 cells[1]
Concentration: 5 μM
Incubation Time: 72 hours
Result: Showed anti-Hh(Hedgehog signaling) activity and anti-proliferative activity.

Cell Proliferation Assay

Cell Line: ASZ001 cells[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: After a 20-h incubation with HSP70-IN-3, expression of Gli1 mRNA was almost completely abolished.

分子量

883.23

Formula

C48H78N6O7S
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]. Wen J, et al. Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma. Eur J Med Chem. 2022;228:114005.

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

HSP70-IN-3

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。

HSP70-IN-3 

HSP70-IN-3 是一种有效的热休克蛋白 (HSP70) 抑制剂 (ASZ001 和 C3H10T1/2 的 IC50 分别为1.1和1.9 μM)。HSP70-IN-3 具有抗 Hedgehog 信号转导通路活性和抗增殖活性，并降低致癌转录因子 GLI1 的表达。

HSP70-IN-3

HSP70-IN-3 Chemical Structure

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

HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1[1].

IC50 & Target

IC50: 1.1 μM (HSP70) in ASZ001, 1.9 μM (HSP70) in C3H10T1/2[1]
体外研究
(In Vitro)

HSP70-IN-3 (compound 8) (5 μM; 72 hours) has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity in ASZ001 cells[1].
HSP70-IN-3 can almost completely abolish the expression of Gli1 mRNA in ASZ001 cells after 20-hour incubation[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.

Cell Proliferation Assay

Cell Line: ASZ001 cells[1]
Concentration: 5 μM
Incubation Time: 72 hours
Result: Showed anti-Hh(Hedgehog signaling) activity and anti-proliferative activity.

Cell Proliferation Assay

Cell Line: ASZ001 cells[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: After a 20-h incubation with HSP70-IN-3, expression of Gli1 mRNA was almost completely abolished.

分子量

883.23

Formula

C48H78N6O7S
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]. Wen J, et al. Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma. Eur J Med Chem. 2022;228:114005.

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

CCT018159

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。

CCT018159 

CCT018159 是一种 3,4-二芳基吡唑间苯二酚，一种 ATP 竞争性 HSP90 ATPase 活性抑制剂，对人 Hsp90β 和酵母 Hsp90 的 IC50 分别为 3.2 和 6.6 µM。CCT018159 引起与 G1 期阻滞相关的细胞细胞抑制并诱导细胞凋亡。CCT018159 抑制与侵袭和血管生成有关的关键内皮细胞和肿瘤细胞功能。

CCT018159

CCT018159 Chemical Structure

CAS No. : 171009-07-7

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

CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis[1].

IC50 & Target[1]

human Hsp90β

3.2 μM (IC50)

yeast Hsp90

6.6 μM (IC50)

分子量

352.38

Formula

C20H20N2O4
CAS 号

171009-07-7
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]. Swee Y Sharp, et al. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Res. 2007 Mar 1;67(5):2206-16.

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

CCT018159

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。

CCT018159 

CCT018159 是一种 3,4-二芳基吡唑间苯二酚，一种 ATP 竞争性 HSP90 ATPase 活性抑制剂，对人 Hsp90β 和酵母 Hsp90 的 IC50 分别为 3.2 和 6.6 µM。CCT018159 引起与 G1 期阻滞相关的细胞细胞抑制并诱导细胞凋亡。CCT018159 抑制与侵袭和血管生成有关的关键内皮细胞和肿瘤细胞功能。

CCT018159

CCT018159 Chemical Structure

CAS No. : 171009-07-7

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生物活性

CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis[1].

IC50 & Target[1]

human Hsp90β

3.2 μM (IC50)

yeast Hsp90

6.6 μM (IC50)

分子量

352.38

Formula

C20H20N2O4
CAS 号

171009-07-7
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]. Swee Y Sharp, et al. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Res. 2007 Mar 1;67(5):2206-16.

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CCT018159

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。

CCT018159 

CCT018159 是一种 3,4-二芳基吡唑间苯二酚，一种 ATP 竞争性 HSP90 ATPase 活性抑制剂，对人 Hsp90β 和酵母 Hsp90 的 IC50 分别为 3.2 和 6.6 µM。CCT018159 引起与 G1 期阻滞相关的细胞细胞抑制并诱导细胞凋亡。CCT018159 抑制与侵袭和血管生成有关的关键内皮细胞和肿瘤细胞功能。

CCT018159

CCT018159 Chemical Structure

CAS No. : 171009-07-7

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

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生物活性

CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis[1].

IC50 & Target[1]

human Hsp90β

3.2 μM (IC50)

yeast Hsp90

6.6 μM (IC50)

分子量

352.38

Formula

C20H20N2O4
CAS 号

171009-07-7
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]. Swee Y Sharp, et al. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Res. 2007 Mar 1;67(5):2206-16.

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

Hsp90-Cdc37-IN-3

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。

Hsp90-Cdc37-IN-3 

Hsp90-Cdc37-IN-3 (Compound 9) 是一种具有抗癌活性 (anticancer) 的新型 celastrol−imidazole 衍生物。Hsp90-Cdc37-IN-3 通过共价结合抑制 Hsp90−Cdc37，诱导细胞凋亡 (apoptosis)。

Hsp90-Cdc37-IN-3

Hsp90-Cdc37-IN-3 Chemical Structure

CAS No. : 2361009-68-7

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

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生物活性

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].

IC50 & Target

Hsp90-Cdc37

 

体外研究
(In Vitro)

Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values of 0.54, 0.59, 0.57, and 0.57 µM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively[1].
Hsp90-Cdc37-IN-3 (0-5 µM, 12 h) inhibits Hsp90−Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37[1].
Hsp90-Cdc37-IN-3 (0-0.8 µM, 48 h) induces apoptosis significantly in A549 cells[1].
Hsp90-Cdc37-IN-3 (0-0.4 µM, 24 h) arrests the cell cycle in the G0/G1 phase in a dose-dependent manner[1].

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

Western Blot Analysis[1]

Cell Line: A549
Concentration: 1.25, 2.5, and 5 µM
Incubation Time: 12 h
Result: Downregulated the levels of Hsp90−Cdc37 clients (p-Akt and Cdk4) in a dose-dependent manner, and the levels of apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3, and cleaved PARP) were significantly regulated.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 0.2, 0.4, and 0.8 μM
Incubation Time: 48 h
Result: Induced apoptosis significantly.

Cell Cycle Analysis[1]

Cell Line: A549
Concentration: 0.1, 0.2, and 0.4 μM
Incubation Time: 24 h
Result: Arrested the cell cycle in the G0/G1 phase in a dose-dependent manner.

体内研究
(In Vivo)

Hsp90-Cdc37-IN-3 (Compound 9) (0-1 mg/kg; i.p.; once a day, 21 days) shows strong antitumor activity with no significant toxicity[1].

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

Animal Model: Female BALB/c nude mice at 6 weeks old[1].
Dosage: 0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107 in 100 μL of PBS for each mouse).
Administration: Intraperitoneal injection, once a day, 21 days
Result: Decreased tumor weight and enhanced TIR without show toxicity.

分子量

638.19

Formula

C35H44ClN3O6
CAS 号

2361009-68-7
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]. Na Li, et al. Discovery of Novel Celastrol-Imidazole Derivatives with Anticancer Activity In Vitro and In Vivo. J Med Chem. 2022 Mar 24;65(6):4578-4589.

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

Hsp90-Cdc37-IN-3

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。

Hsp90-Cdc37-IN-3 

Hsp90-Cdc37-IN-3 (Compound 9) 是一种具有抗癌活性 (anticancer) 的新型 celastrol−imidazole 衍生物。Hsp90-Cdc37-IN-3 通过共价结合抑制 Hsp90−Cdc37，诱导细胞凋亡 (apoptosis)。

Hsp90-Cdc37-IN-3

Hsp90-Cdc37-IN-3 Chemical Structure

CAS No. : 2361009-68-7

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

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].

IC50 & Target

Hsp90-Cdc37

 

体外研究
(In Vitro)

Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values of 0.54, 0.59, 0.57, and 0.57 µM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively[1].
Hsp90-Cdc37-IN-3 (0-5 µM, 12 h) inhibits Hsp90−Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37[1].
Hsp90-Cdc37-IN-3 (0-0.8 µM, 48 h) induces apoptosis significantly in A549 cells[1].
Hsp90-Cdc37-IN-3 (0-0.4 µM, 24 h) arrests the cell cycle in the G0/G1 phase in a dose-dependent manner[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.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 1.25, 2.5, and 5 µM
Incubation Time: 12 h
Result: Downregulated the levels of Hsp90−Cdc37 clients (p-Akt and Cdk4) in a dose-dependent manner, and the levels of apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3, and cleaved PARP) were significantly regulated.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 0.2, 0.4, and 0.8 μM
Incubation Time: 48 h
Result: Induced apoptosis significantly.

Cell Cycle Analysis[1]

Cell Line: A549
Concentration: 0.1, 0.2, and 0.4 μM
Incubation Time: 24 h
Result: Arrested the cell cycle in the G0/G1 phase in a dose-dependent manner.

体内研究
(In Vivo)

Hsp90-Cdc37-IN-3 (Compound 9) (0-1 mg/kg; i.p.; once a day, 21 days) shows strong antitumor activity with no significant 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: Female BALB/c nude mice at 6 weeks old[1].
Dosage: 0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107 in 100 μL of PBS for each mouse).
Administration: Intraperitoneal injection, once a day, 21 days
Result: Decreased tumor weight and enhanced TIR without show toxicity.

分子量

638.19

Formula

C35H44ClN3O6
CAS 号

2361009-68-7
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]. Na Li, et al. Discovery of Novel Celastrol-Imidazole Derivatives with Anticancer Activity In Vitro and In Vivo. J Med Chem. 2022 Mar 24;65(6):4578-4589.

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

Hsp90-Cdc37-IN-3

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。

Hsp90-Cdc37-IN-3 

Hsp90-Cdc37-IN-3 (Compound 9) 是一种具有抗癌活性 (anticancer) 的新型 celastrol−imidazole 衍生物。Hsp90-Cdc37-IN-3 通过共价结合抑制 Hsp90−Cdc37，诱导细胞凋亡 (apoptosis)。

Hsp90-Cdc37-IN-3

Hsp90-Cdc37-IN-3 Chemical Structure

CAS No. : 2361009-68-7

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

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].

IC50 & Target

Hsp90-Cdc37

 

体外研究
(In Vitro)

Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values of 0.54, 0.59, 0.57, and 0.57 µM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively[1].
Hsp90-Cdc37-IN-3 (0-5 µM, 12 h) inhibits Hsp90−Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37[1].
Hsp90-Cdc37-IN-3 (0-0.8 µM, 48 h) induces apoptosis significantly in A549 cells[1].
Hsp90-Cdc37-IN-3 (0-0.4 µM, 24 h) arrests the cell cycle in the G0/G1 phase in a dose-dependent manner[1].

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

Western Blot Analysis[1]

Cell Line: A549
Concentration: 1.25, 2.5, and 5 µM
Incubation Time: 12 h
Result: Downregulated the levels of Hsp90−Cdc37 clients (p-Akt and Cdk4) in a dose-dependent manner, and the levels of apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3, and cleaved PARP) were significantly regulated.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 0.2, 0.4, and 0.8 μM
Incubation Time: 48 h
Result: Induced apoptosis significantly.

Cell Cycle Analysis[1]

Cell Line: A549
Concentration: 0.1, 0.2, and 0.4 μM
Incubation Time: 24 h
Result: Arrested the cell cycle in the G0/G1 phase in a dose-dependent manner.

体内研究
(In Vivo)

Hsp90-Cdc37-IN-3 (Compound 9) (0-1 mg/kg; i.p.; once a day, 21 days) shows strong antitumor activity with no significant toxicity[1].

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

Animal Model: Female BALB/c nude mice at 6 weeks old[1].
Dosage: 0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107 in 100 μL of PBS for each mouse).
Administration: Intraperitoneal injection, once a day, 21 days
Result: Decreased tumor weight and enhanced TIR without show toxicity.

分子量

638.19

Formula

C35H44ClN3O6
CAS 号

2361009-68-7
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]. Na Li, et al. Discovery of Novel Celastrol-Imidazole Derivatives with Anticancer Activity In Vitro and In Vivo. J Med Chem. 2022 Mar 24;65(6):4578-4589.

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

Hsp90-Cdc37-IN-1

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。

Hsp90-Cdc37-IN-1 

Hsp90-Cdc37-IN-1是 Hsp90-Cdc37 相互作用破坏剂，其抑制细胞迁移和逆转抗药性，IC50 为140nM。

Hsp90-Cdc37-IN-1

Hsp90-Cdc37-IN-1 Chemical Structure

CAS No. : 2227303-22-0

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

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生物活性

Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.

IC50 & Target

IC50: 140 nM (Hsp90-Cdc37)[1]
分子量

748.99

Formula

C43H57FN2O6S
CAS 号

2227303-22-0
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]. Jin L, et al. Discovery of 18β-glycyrrhetinic acid conjugated aminobenzothiazole derivatives as Hsp90-Cdc37 interaction disruptors that inhibit cell migration and reverse drug resistance. Bioorg Med Chem. 2018 May 1;26(8):1759-1775.

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

PROTAC HSP90 degrader BP3

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。

PROTAC HSP90 degrader BP3 

PROTAC HSP90 degrader BP3 以 CRBN 依赖性方式有效且选择性地降解 HSP90。PROTAC HSP90 degrader BP3对 MCF-7 细胞中的 HSP90 蛋白有一定的降解作用 (DC50=0.99 µM)。PROTAC HSP90 degrader BP3 抑制乳腺癌细胞的生长。

PROTAC HSP90 degrader BP3

PROTAC HSP90 degrader BP3 Chemical Structure

CAS No. : 2669072-88-0

规格 价格 是否有货
5 mg ￥6500 询问价格 & 货期
10 mg ￥10200 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 µM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell[1].

IC50 & Target

HSP90

 

Cereblon

 

体外研究
(In Vitro)

PROTAC HSP90 degrader BP3 (compound 16b) (72 h) inhibits the growth of breast cancer cells (IC50=0.63 µM in MCF-7 cells, IC50=3.53 µM in MDA-MB-231 cells, IC50=0.61 µM in 4T1 cells, IC50=2.95 µM in MDA-MB-468 cells)[1].
PROTAC HSP90 degrader BP3 (2 µM; 6 h) shows degradation activity in the MCF-7 cells (DC50=0.99 µM)[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.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2 µM
Incubation Time: 6 h
Result: Showed degradation activity in the MCF-7 cells (DC50=0.99 µM).

Cell Viability Assay[1]

Cell Line: 4T1, MDA-MB-468 cells
Concentration: 0.01, 1, 100, 10000 µM
Incubation Time: 72 h
Result: Inhibited the growth of cancer cells (IC50=0.61 µM in 4T1 cells, IC50=2.95 µM in MDA-MB-468 cells).

体内研究
(In Vivo)

PROTAC HSP90 degrader BP3 (40 mg/kg; i.p., daily for 12 days) inhibits tumor growth and the tumor inhibition rate is 76.41%[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: 6- to 8-week-old female BALB/c mice[1]
Dosage: 40 mg/kg
Administration: i.p., daily, 12 days
Result: Inhibited tumor growth and the tumor inhibition rate was 76.41%.

分子量

641.08

Formula

C32H29ClN8O5
CAS 号

2669072-88-0
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]. Liu Q, et al. Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer. Eur J Med Chem. 2022, 228:114013.

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

VER-155008

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。

VER-155008  纯度: 99.87%

VER-155008 是一种 Hsp70 的抑制剂，对 Hsp70，Hsc70 和 Grp7 的 IC50 值分别为 0.5 μM，2.6 μM 和 2.6 μM，对 Hsp70 的 Kd 值为 0.3 μM。

VER-155008

VER-155008 Chemical Structure

CAS No. : 1134156-31-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥857 In-stock
5 mg ￥700 In-stock
10 mg ￥860 In-stock
50 mg ￥2950 In-stock
100 mg ￥5200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VER-155008 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Nucleotide Compound Library
  • Cytoskeleton Compound Library
  • Targeted Diversity Library

生物活性

VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.

IC50 & Target[1]

HSP70

0.5 μM (IC50)

HSC70

2.6 μM (IC50)

Grp78

2.6 μM (IC50)

体外研究
(In Vitro)

VER-155008 is an inhibitor of Hsc70 and Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, a with a Kd of 0.3 μM for Hsp70, but shows no activities against Hsp90, with an IC50 of >200 μM. VER-155008 inhibits the proliferation of a variety of human colon and breast tumor cell lines, such as BT474, MB-468, HCT116 and HT29 cells, with GI50s of 10.4 μM, 14.4 μM, 5.3 μM, and 12.8 μM, respectively. VER-155008 (5-40 μM) induces client protein degradation in HCT116 and BT474 carcinoma cells. VER-155008 also induces apoptosis in human tumor cell lines[1]. VER-155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons[2]. VER-155008 (10 μM or 25 μM) inhibits Hsp70 and suppresses the proliferation of LNCaP95 cells. VER-155008 also reduces full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7) protein expression[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.
体内研究
(In Vivo)

VER-155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice[1]. VER-155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice[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

556.40

Formula

C25H23Cl2N7O4
CAS 号

1134156-31-2
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 : ≥ 37 mg/mL (66.50 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 1.7973 mL 8.9863 mL 17.9727 mL
5 mM 0.3595 mL 1.7973 mL 3.5945 mL
10 mM 0.1797 mL 0.8986 mL 1.7973 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 (4.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.49 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 (4.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.49 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 (4.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.49 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]. Massey AJ, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45.

    [2]. Yang X, et al. Heat Shock Cognate 70 Inhibitor, VER-155008, Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimer’s Disease. Front Pharmacol. 2018 Jan 30;9:48.

    [3]. Kita K, et al. Heat shock protein 70 inhibitors suppress androgen receptor expression in LNCaP95 prostate cancer cells. Cancer Sci. 2017 Sep;108(9):1820-1827.
Cell Assay
[2]

Embryos are removed from a pregnant ddY mouse at 14 days of gestation. Cells are treated with or without 10 μM Aβ25-35 for 3 days, followed by the addition of 0.05, 0.5, or 5 μM VER-155008 or vehicle solution (0.1% DMSO) for 4 days. The Aβ25-35 is incubated at 37°C for 4 days prior to treatment to facilitate aggregation. The cells are fixed with 4% paraformaldehyde and immunostained at 4°C for 24 h with antibodies against the axonal marker, mouse phosphorylated neurofilament heavy subunit, and against the neuronal marker, rabbit microtubule-associated protein 2. Alexa Fluor 488-conjugated goat anti-mouse IgG (1:400) and Alexa Fluor 568-conjugated goat anti-rabbit IgG (1:400) are used as secondary antibodies. Fluorescence images (864.98 μm × 645.62 μm) are captured using a fluorescence microscopy system. The lengths of the pNF-H-positive axons are measured using MetaMorph version 7.8[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
[1]

Female BALB/c mice are dosed intravenously with 25 mg/kg VER-155008 into the lateral tail vein as a solution in 10% DMSO/5% Tween 80/85% saline (v/v/v). Animals are sacrificed at 5, 15 and 30 min, 1, 2, 4 and 6 h post dose[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.
参考文献

  • [1]. Massey AJ, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45.

    [2]. Yang X, et al. Heat Shock Cognate 70 Inhibitor, VER-155008, Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimer’s Disease. Front Pharmacol. 2018 Jan 30;9:48.

    [3]. Kita K, et al. Heat shock protein 70 inhibitors suppress androgen receptor expression in LNCaP95 prostate cancer cells. Cancer Sci. 2017 Sep;108(9):1820-1827.

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

HSP70-IN-1

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。

HSP70-IN-1  纯度: 98.01%

HSP70-IN-1是一种热休克蛋白 (HSP) 抑制剂; 抑制Kasumi-1细胞的生长的IC50值为2.3 μM。

HSP70-IN-1

HSP70-IN-1 Chemical Structure

CAS No. : 1268273-90-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3373 In-stock
1 mg ￥1100 In-stock
5 mg ￥3300 In-stock
10 mg ￥5000 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

HSP70-IN-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Cytoskeleton Compound Library
  • Targeted Diversity Library

生物活性

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

IC50 & Target[1]

HSP70

 

Caspase-3/7

1.9 μM (IC50, MOLM13 cells)

体外研究
(In Vitro)

The heat shock protein 70 (Hsp70) is a molecular chaperone which plays an important function in protein homeostasis as well as in cell signaling and survival. Hsp70 is frequently overexpressed in cancer, where the elevated expression is furthermore believed to be a cause of or to lead to resistance to chemotherapy and other treatments. HSP70-IN-1 interferes with the formation of functional Hsp70-HOP-Hsp90 machinery by its ability to dose-dependently alter the megacomplex components and to destabilize an Hsp70-Hsp90 machinery client, Raf-1. In cells, the refolding of heat-denatured luciferase by endogenous as well as transfected Hsp70 is inhibited by HSP70-IN-1. HSP70-IN-1 also results in induction of apoptosis in cancer cells. Addition of HSP70-IN-1to cancer cells dose-dependently alters the formation of the Hsp70-HOP complex, a phenomenon associated with their destabilization and reduction in half-life[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.
分子量

464.58

Formula

C24H28N6O2S
CAS 号

1268273-90-0
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 (107.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1525 mL 10.7624 mL 21.5248 mL
5 mM 0.4305 mL 2.1525 mL 4.3050 mL
10 mM 0.2152 mL 1.0762 mL 2.1525 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 (5.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.38 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 (5.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.38 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 (5.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.38 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]. Taldone T, et al. Heat shock protein 70 inhibitors. 2. 2,5′-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014 Feb 27;57(4):1208-24.

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