2. Apoptosis Cell Cycle/DNA Damage
  3. Apoptosis CDK
  4. CDK9-IN-33

CDK9-IN-33 (compound C35) 是一种有效的、选择性和具有口服活性的 CDK9 抑制剂，对 CDK9、CDK7、CDK2、CDK4、CDK6 的 IC50 值分别为 17.44、160、316.30、1771.00、>10000 nM。CDK9-IN-33 诱导细胞凋亡 (apoptosis)。CDK9-IN-33 降低 RPB1 CTD Ser2、RPB1 和 MCL1 的蛋白表达。CDK9-IN-33 显示出抗肿瘤活性。

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CDK9-IN-33 Chemical Structure

CDK9-IN-33 Chemical Structure

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CDK9-IN-33 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity[1].

IC50 & Target[1]

CDK9

17.44 nM (IC50)

CDK7

160 nM (IC50)

CDK2

316.30 nM (IC50)

CDK4

1771.00 nM (IC50)

CDK6

>10000 nM (IC50)

体外研究
(In Vitro)

CDK9-IN-33 (compound C35) (0, 0.01, 0.1, 1 µM; 24 h) 降低 RPB1 CTD Ser2、RPB1、MCL1 的蛋白质表达，并增加裂解 PARP 的表达[1]。
CDK9-IN-33 (0, 0.01, 0.1, 1 µM) 降低 MCL1 基因的 mRNA 表达水平[1]。
CDK9-IN-33 (0, 0.01, 0.1, 1 µM; 72 h) 以剂量依赖性方式诱导细胞凋亡[1]。

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

CDK9-IN-33 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells
Concentration:
Incubation Time: 4 days
Result: Showed antiproliferation potential for MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells with IC50 values of 5.9, 10.05, 5.61, 20.08, 8.98, 24.38 nM, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.01, 0.1, 1 µM
Incubation Time: 24 h
Result: Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.01, 0.1, 1 µM
Incubation Time: 24 h
Result: Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.

Apoptosis Analysis[1]

Cell Line: 4T1 cells
Concentration: 0, 0.01, 0.1, 1 µM
Incubation Time: 72 h
Result: Induced apoptosis in a dose-dependent manner.
体内研究
(In Vivo)

CDK9-IN-33 (10 mg/kg; p.o.; daily for 10 days) 在小鼠中显示出抗肿瘤活性[1]。
药代动力学分析[1]。

Cmpd T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (h·ng/mL) AUCt–∞ (h·ng/mL) CL (mL/min/kg) MRT0–∞ (h) Vss (mL/kg) F (%)
C35 (p.o.) 0.68 0.5 2867 4349 4350 - 1.43 - 68.9
C35 (i.v.) 0.36 - - 1578 1578 52.9 0.33 1033 -

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

437.54

Formula

C23H31N7O2
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.
纯度 & 产品资料
参考文献

CDK9-IN-33 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

CDK9-IN-33ApoptosisCDKCyclin dependent kinaseorally activeantiproliferationRPB1 CTD Ser2RPB1MCL1MDA-MB-231 cellsapoptosisanti-tumorInhibitorinhibitorinhibit

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