标签归档：pdk

PDK4-IN-1 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。

PDK4-IN-1 hydrochloride  纯度: 99.48%

PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，也是一种有效的，口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂，IC50 值为 84 nM。PDK4-IN-1 hydrochloride 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病，抗癌和抗过敏作用。

PDK4-IN-1 hydrochloride

PDK4-IN-1 hydrochloride Chemical Structure

CAS No. : 2310262-11-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4180 In-stock
5 mg ￥3800 In-stock
10 mg ￥5800 In-stock
50 mg ￥16500 In-stock
100 mg ￥23500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PDK4-IN-1 hydrochloride 相关产品

•相关化合物库:

  • Natural Product Like Compound Library
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Diabetes Related Compound Library
  • Glycolysis Compound Library
  • Orally Active Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Mitochondria-Targeted Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity[1].

IC50 & Target

IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))[1]
体外研究
(In Vitro)

PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1[1].
PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis[1].
PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α[1].
10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells[1].
PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1[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 Viability Assay[1]

Cell Line: HCT116 and RKO cells
Concentration: 50 μM
Incubation Time: 0 hour, 24 hours, 48 hours, 72hours
Result: Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.

Apoptosis Analysis[1]

Cell Line: HCT116 and RKO cells
Concentration: 10 μM, 25 μM, 50 μM
Incubation Time: 24 hours
Result: Dose-dependently increased apoptosis.

Western Blot Analysis[1]

Cell Line: HEK293T human embryonic kidney cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Inhibited phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α.

体内研究
(In Vivo)

PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance[1].
Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs[1].
The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats[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: C57BL/6J mice (8-week old) fed with high-fat diet[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 1 week
Result: Significantly improved glucose tolerance.

分子量

393.87

Formula

C22H20ClN3O2
CAS 号

2310262-11-2
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (317.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5389 mL 12.6945 mL 25.3891 mL
5 mM 0.5078 mL 2.5389 mL 5.0778 mL
10 mM 0.2539 mL 1.2695 mL 2.5389 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 (sealed storage, away from moisture)。-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： 0.5% CMC-Na/saline water

    Solubility: 20 mg/mL (50.78 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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
*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 D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588.

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

(R)-PS210

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。

(R)-PS210  纯度: 98.20%

(R)-PS210 是 PS210 的 R 对映异构体 (化合物 4h-eutomer)，是 PDK1 的底物选择性变构激活剂，AC50 值为 1.8 μM。(R)-PS210 靶向 PDK1 的 PIF 结合口袋。PIF: 蛋白激酶 C 相关激酶 2 (PRK2) 相互作用片段。

(R)-PS210

(R)-PS210 Chemical Structure

CAS No. : 1410101-89-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥2500 In-stock
10 mg ￥3900 In-stock
25 mg ￥7800 In-stock
50 mg ￥12500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

(R)-PS210 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment[1].

IC50 & Target

AC50: 1.8 μM (PDK1)[1]
体外研究
(In Vitro)

(R)-PS210 displays an AC50 value of 1.8 μM towards PDK1 in a Cell-Free Kinase Activity Assay. And the maximum activation of PDK1 compared to DMSO control of (R)-PS210 is 5.5 fold[1].

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

380.31

Formula

C19H15F3O5
CAS 号

1410101-89-1
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 : 230 mg/mL (604.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6294 mL 13.1472 mL 26.2943 mL
5 mM 0.5259 mL 2.6294 mL 5.2589 mL
10 mM 0.2629 mL 1.3147 mL 2.6294 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: ≥ 5.75 mg/mL (15.12 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (15.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 57.5 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: ≥ 5.75 mg/mL (15.12 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (15.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 57.5 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: ≥ 5.75 mg/mL (15.12 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (15.12 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 57.5 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Wilhelm A, et al. 2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: development and prodrug concept.J Med Chem. 2012 Nov 26;55(22):9817-30.

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

MP7(Synonyms: PDK1 inhibitor)

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。

MP7 (Synonyms: PDK1 inhibitor) 纯度: 99.83%

MP7 (PDK1 inhibitor) 是一种磷酸肌醇依赖性激酶-1 (PDK1) 抑制剂。

MP7(Synonyms: PDK1 inhibitor)

MP7 Chemical Structure

CAS No. : 1001409-50-2

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 ￥1406 In-stock
5 mg ￥1237 In-stock
10 mg ￥2288 In-stock
50 mg ￥8602 In-stock
100 mg ￥13020 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MP7 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.

IC50 & Target

PDK1[1]
体外研究
(In Vitro)

Cell counting of U87MG-derived glioma stem cells (GSCs) confirms that Alisertib and, to a minor extent, MP7 (PDK1 inhibitor) are able to decrease the number of viable cells. When combined together, GSC viability is further reduced with respect to single-treated cells. As observed in U87MG cells, when used at the highest concentrations (i.e., 1.5 μM Alisertib and 2.5 μM MP7), a significant enhancement in the number of dead cells is evidenced. Following 72 h treatment, MP7 alone does not show a significant inhibition of glioblastoma multiforme (GBM) proliferation. MP7 has been shown to have only minimal effects on monolayer cell growth in several cancer cell lines, with IC50 values in the micromolar range[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

516.50

Formula

C28H22F2N4O4
CAS 号

1001409-50-2
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 : ≥ 100 mg/mL (193.61 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 1.9361 mL 9.6805 mL 19.3611 mL
5 mM 0.3872 mL 1.9361 mL 3.8722 mL
10 mM 0.1936 mL 0.9681 mL 1.9361 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: ≥ 2.75 mg/mL (5.32 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.32 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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: ≥ 2.75 mg/mL (5.32 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.32 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 27.5 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]. Daniele S, et al. Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells. ACS Chem Neurosci. 2017 Jan 18;8(1):100-114.
Cell Assay
[1]

The human GBM cells (i.e., U87MG, U343MG, or ANGM-CSS) or the respective GSCs are seeded and incubated for the indicated times with the indicated concentrations of SA16 (1 nM to 100 μM), MP7 (2.5 nM, 25 nM, 250 nM and 2.5 μM), or Alisertib. When indicated, cells are treated with MP7 and Alisertib in combination. To verify GSC chemoresistance, U87MG or GSCs are incubated with 50 μM TMZ for 72 h. For the long-term treatment of cells, NSC or complete medium containing drugs is replaced every 3 days. Cell proliferation is determined using the MTS assay: the dehydrogenase activity in active mitochondria reduces MTS to the soluble formazan product, whose absorbance at 490 nm is measured with an automated plate reader. The mean background from each test condition is subtracted, and the data are expressed as the percentage of untreated cells (control). IC50 values are derived from the sigmoid dose-response curve. The percentage of inhibition is calculated as 100% minus the percentage of cell proliferation[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]. Daniele S, et al. Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells. ACS Chem Neurosci. 2017 Jan 18;8(1):100-114.

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

PDK4-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。

PDK4-IN-1 

PDK4-IN-1 是一种蒽醌衍生物，也是一种有效的，口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂，IC50 值为 84 nM。PDK4-IN-1 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 具有抗糖尿病，抗癌和抗过敏作用。

PDK4-IN-1

PDK4-IN-1 Chemical Structure

CAS No. : 2310262-10-1

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

* Please select Quantity before adding items.

PDK4-IN-1 的其他形式现货产品:

PDK4-IN-1 hydrochloride

生物活性

PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].

IC50 & Target

IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))[1]
体外研究
(In Vitro)

PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1[1].
PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis[1].
PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α[1].
10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells[1].
PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1[1].

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

Cell Viability Assay[1]

Cell Line: HCT116 and RKO cells
Concentration: 50 μM
Incubation Time: 0 hour, 24 hours, 48 hours, 72hours
Result: Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.

Apoptosis Analysis[1]

Cell Line: HCT116 and RKO cells
Concentration: 10 μM, 25 μM, 50 μM
Incubation Time: 24 hours
Result: Dose-dependently increased apoptosis.

Western Blot Analysis[1]

Cell Line: HEK293T human embryonic kidney cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Inhibited phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α.

体内研究
(In Vivo)

PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance[1].
Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs[1].
The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats[1].

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

Animal Model: C57BL/6J mice (8-week old) fed with high-fat diet[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 1 week
Result: Significantly improved glucose tolerance.

分子量

357.41

Formula

C22H19N3O2
CAS 号

2310262-10-1
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]. Lee D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588.

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-246608

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-246608  纯度: 98.92%

VER-246608 是一种有效的，ATP 竞争性的丙酮酸脱氢酶激酶 (PDK) 抑制剂，抑制 PDK-1，PDK-3，PDK-2，和 PDK-4，IC50 分别为 35 nM，40 nM，84 nM 和 91 nM。

VER-246608

VER-246608 Chemical Structure

CAS No. : 1684386-71-7

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 ￥1710 In-stock
5 mg ￥1400 In-stock
10 mg ￥2200 In-stock
25 mg ￥4200 In-stock
50 mg ￥6400 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VER-246608 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Glycolysis Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Mitochondria-Targeted Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.

IC50 & Target

IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)[1]
体外研究
(In Vitro)

VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK. VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range. In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser293 residue of E1α (phosphorylated by all four PDK isozymes) with IC50 values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth[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

552.96

Formula

C28H23ClF2N4O4
CAS 号

1684386-71-7
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 (180.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8084 mL 9.0422 mL 18.0845 mL
5 mM 0.3617 mL 1.8084 mL 3.6169 mL
10 mM 0.1808 mL 0.9042 mL 1.8084 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 (4.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.52 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 (4.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.52 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]. Moore JD, et al. VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget. 2014 Dec 30;5(24):12862-76.
Kinase Assay
[1]

DELFIA assay reagents (assay buffer, wash buffer, enhancement solution and anti-rabbit IgG-Eu-N1 secondary antibody) and plates are used. Test compounds are subjected to a 10 point tripling dilution in DMSO, diluted in MOPS buffer (60 mM MOPS pH7.2, 15 mM Magnesium acetate, 60 mM KCl) and added to the enzyme mix (10 nM PDK-1, 2 and 3 or 20 nM PDK-4, 300 nM E1, 0.1 mg/mL BSA, 1 mM DTT) in 96-well V-bottom plates. The reaction is initiated by the addition of ATP to a final concentration of 5 μM followed by a 1 h incubation at 30°C. The reaction is then stopped by the addition of STOP solution (50 mM Carbonate-Bicarbonate Buffer, pH 9.6), and then transferred to 96 well DEFLIA yellow plates. The plates are then sealed and incubated o/n at 4°C. Detection and quantification of p(Ser293)E1α levels is then achieved through incubation with anti-p(Ser293)E1α primary antibody followed by anti-rabbit secondary IgG-Eu-N1 antibody and addition of enhancement solution. The time-resolved fluorescent signal is then measured using a Victor2 plate reader. The data is fitted by non-linear regression using XLFIT4 within a custom ABASE (IDBS) protocol in order to determine IC50 values[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 Assay
[1]

Compound cytotoxicity is determined using the Sulforhodamine B assay for cells cultured as a monolayer. For spheroid growth experiments, PC-3 cells are seeded (500 cells/well) into 96 well round bottom plates in RPMI-1640 media containing 2.5% (w/v) Matrigel. The resultant spheroids are treated with VER-246608 (2.5, 5, 10, 20, and 40 μM) 48 h post-seeding. Spheroid volumes are determined by obtaining diameter measurements from images taken on a Zeiss Axiovert 200 M inverted microscope using the axiovision software[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]. Moore JD, et al. VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget. 2014 Dec 30;5(24):12862-76.

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

PS210

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。

PS210  纯度: 98.00%

PS210 是一种针对 PDK1 的 PIF 结合口袋的有效且选择性的 PDK1 激活剂。PS210 对其他蛋白激酶 (包括 PDK1 下游信号传导成分，如 S6K，PKB/Akt 或 GSK3) 无活性。在细胞中，PS210 的前药 PS423 可作为 PDK1 的底物选择性抑制剂，抑制 S6K 的磷酸化和活化。

PS210

PS210 Chemical Structure

CAS No. : 1221962-86-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥880 In-stock
5 mg ￥800 In-stock
10 mg ￥1300 In-stock
25 mg ￥2500 In-stock
50 mg ￥4500 In-stock
100 mg ￥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PS210 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K[1][2].

IC50 & Target

Kd: 3 μM (PDK1)[2]
体外研究
(In Vitro)

When PS210 induces a stabilization of PDK1 to the temperature gradien, PS210 stabilized the residue Arg131, located opposite to the helix a-B at the other extreme of the helix a-C. Thus, the residues forming part of the phosphate-binding site appear to be a fixed point that allows for the relative movement of the helices in the process of PDK1 activation[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

380.31

Formula

C19H15F3O5
CAS 号

1221962-86-2
运输条件

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

DMSO : 100 mg/mL (262.94 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6294 mL 13.1472 mL 26.2943 mL
5 mM 0.5259 mL 2.6294 mL 5.2589 mL
10 mM 0.2629 mL 1.3147 mL 2.6294 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 (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 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 (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 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 (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 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]. Busschots K, et al. Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site. Chem Biol. 2012 Sep 21;19(9):1152-63.

    [2]. Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5.

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

PDK1-IN-RS2

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。

PDK1-IN-RS2 

PDK1-IN-RS2 是一种肽对接基序 (PIFtide) 的模拟物，也是一种底物选择性 PDK1 抑制剂，Kd 为 9 μM。PDK1-IN-RS2 抑制 PDK1 对下游激酶 S6K1 的激活。

PDK1-IN-RS2

PDK1-IN-RS2 Chemical Structure

CAS No. : 1643958-89-7

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

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1[1].

IC50 & Target

Kd: 9 μM (PDK1)[1]
体外研究
(In Vitro)

PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions[1].

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

380.89

Formula

C15H9ClN2O2S3
CAS 号

1643958-89-7
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]. Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5.

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

PDK1-IN-RS2

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。

PDK1-IN-RS2 

PDK1-IN-RS2 是一种肽对接基序 (PIFtide) 的模拟物，也是一种底物选择性 PDK1 抑制剂，Kd 为 9 μM。PDK1-IN-RS2 抑制 PDK1 对下游激酶 S6K1 的激活。

PDK1-IN-RS2

PDK1-IN-RS2 Chemical Structure

CAS No. : 1643958-89-7

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

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1[1].

IC50 & Target

Kd: 9 μM (PDK1)[1]
体外研究
(In Vitro)

PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions[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

380.89

Formula

C15H9ClN2O2S3
CAS 号

1643958-89-7
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]. Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5.

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

PDK1-IN-RS2

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。

PDK1-IN-RS2 

PDK1-IN-RS2 是一种肽对接基序 (PIFtide) 的模拟物，也是一种底物选择性 PDK1 抑制剂，Kd 为 9 μM。PDK1-IN-RS2 抑制 PDK1 对下游激酶 S6K1 的激活。

PDK1-IN-RS2

PDK1-IN-RS2 Chemical Structure

CAS No. : 1643958-89-7

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

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1[1].

IC50 & Target

Kd: 9 μM (PDK1)[1]
体外研究
(In Vitro)

PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions[1].

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

380.89

Formula

C15H9ClN2O2S3
CAS 号

1643958-89-7
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]. Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5.

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