2. Metabolic Enzyme/Protease Apoptosis
  3. PDHK Apoptosis
  4. 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。

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PDK4-IN-1 Chemical Structure

PDK4-IN-1 Chemical Structure

CAS No. : 2310262-10-1

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规格 价格 是否有货 数量
1 mg ￥1727
In-stock
5 mg ￥3800
In-stock
10 mg ￥5800
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

Other Forms of PDK4-IN-1:

PDK4-IN-1 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PDK4-IN-1 相关抗体:

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].

MCE 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
性状

固体

颜色

Light yellow to yellow

运输条件

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

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (279.79 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7979 mL 13.9895 mL 27.9791 mL
5 mM 0.5596 mL 2.7979 mL 5.5958 mL
查看完整储备液配制表

* 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 and 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PDK4-IN-1 相关分类

完整储备液配制表

* 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 and 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7979 mL 13.9895 mL 27.9791 mL 69.9477 mL
5 mM 0.5596 mL 2.7979 mL 5.5958 mL 13.9895 mL
10 mM 0.2798 mL 1.3990 mL 2.7979 mL 6.9948 mL
15 mM 0.1865 mL 0.9326 mL 1.8653 mL 4.6632 mL
20 mM 0.1399 mL 0.6995 mL 1.3990 mL 3.4974 mL
25 mM 0.1119 mL 0.5596 mL 1.1192 mL 2.7979 mL
30 mM 0.0933 mL 0.4663 mL 0.9326 mL 2.3316 mL
40 mM 0.0699 mL 0.3497 mL 0.6995 mL 1.7487 mL
50 mM 0.0560 mL 0.2798 mL 0.5596 mL 1.3990 mL
60 mM 0.0466 mL 0.2332 mL 0.4663 mL 1.1658 mL
80 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8743 mL
100 mM 0.0280 mL 0.1399 mL 0.2798 mL 0.6995 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PDK4-IN-12310262-10-1PDHKApoptosisPyruvate dehydrogenase kinasePDH kinasePDK4anticancermetabolitesPDHE1αp-Aktantidiabeticanti-allergicp53BCL-xLBAXPARP1caspase-3Inhibitorinhibitorinhibit

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目录号：
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