2. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR TGF-beta/Smad Epigenetics
  3. CDK GSK-3 PKC
  4. CDK8-IN-12

CDK8-IN-12 是一种具有口服活性的有效 CDK8 抑制剂，Ki 为 14 nM。CDK8-IN-12 对 GSK-3α、GSK-3β、PCK-θ 具有脱靶激酶抑制作用，Ki 分别为 13 nM、4 nM、109 nM。CDK8-IN-12 选择性地对 MV4-11 细胞显示出有效的抗增殖作用。CDK8-IN-12 是一种抗癌剂。

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CDK8-IN-12 Chemical Structure

CDK8-IN-12 Chemical Structure

CAS No. : 2613307-67-6

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规格 价格 是否有货 数量
1 mg ￥952
1 周
5 mg   询价  
10 mg   询价  

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CDK8-IN-12 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

查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

查看 PKC 亚型特异性产品:

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent[1].

IC50 & Target[1]

CDK8

14 nM (Ki)

GSK-3α

13 nM (Ki)

GSK-3β

4 nM (Ki)

PKCθ

109 nM (Ki)

体外研究
(In Vitro)

CDK8-IN-12 (化合物 38) 选择性抑制 MV4-11 急性髓性白血病细胞的增殖，GI50 为 0.36 μM[1]。
CDK8-IN-12 (0.36, 0.72 μM; 2 小时) 显着降低 STAT1 丝氨酸 727 的磷酸化[1]。

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

CDK8-IN-12 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.36, 0.72 μM
Incubation Time: 2 hours
Result: Significantly reduced the phosphorylation of serine 727 on STAT1 at concentrations of their respective 1× GI50 values, but barely affected the level of total STAT1.
体内研究
(In Vivo)

CDK8-IN-12 (化合物 38; 静脉给药; 大鼠 5 mg/kg; 小鼠 2 mg/kg) 对大鼠和小鼠的 T1/2 分别为 0.9 小时和 0.34 小时[1]。

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

381.86

Formula

C21H20ClN3O2
CAS 号
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

CDK8-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

CDK8-IN-122613307-67-6CDKGSK-3PKCCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Protein kinase COrallyGSK-3αGSK-3βPCK-θanti-proliferativeMV4-11 cellanti-cancerInhibitorinhibitorinhibit

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