2. Cell Cycle/DNA Damage Stem Cell/Wnt
  3. CDK β-catenin
  4. CDK8-IN-11 hydrochloride

CDK8-IN-11 hydrochloride 是一种有效的、选择性的 CDK8 抑制剂，IC50 值为 46 nM。CDK8-IN-11 hydrochloride 可抑制 WNT/β-catenin 信号通路。CDK8-IN-11 hydrochloride 可用于结肠癌的研究。

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CDK8-IN-11 hydrochloride Chemical Structure

CDK8-IN-11 hydrochloride Chemical Structure

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CDK8-IN-11 hydrochloride 的其他形式现货产品:

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Other Forms of CDK8-IN-11 hydrochloride:

CDK8-IN-11 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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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

CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer[1].

体外研究
(In Vitro)

CDK8-IN-11 (compound 29, 200 nM) hydrochloride shows inhibitory effects against CDK8 by 73.6% [1].
CDK8-IN-11 (0-50 μM, 48 h) hydrochloride inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) hydrochloride inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) hydrochloride suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].
CDK8-IN-11 (0.5-2 μM, 48 h) hydrochloride increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) hydrochloride reverses Sorafenib (HY-10201) resistance of HCT-116 cells[1].

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

CDK8-IN-11 hydrochloride 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT-116, HHT-29, SW480, CT-26, GES-1 cells
Concentration: 0.08, 0.4, 2, 10, and 50 μM
Incubation Time: 48 h
Result: Inhibited cell proliferation with IC50 values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively.

Western Blot Analysis[1]

Cell Line: HCT-116 cell
Concentration: 0, 1, 2, 4 μM
Incubation Time: 48 h
Result: Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cell
Concentration: 0.5-2 μM
Incubation Time: 48 h
Result: Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells.
体内研究
(In Vivo)

CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) hydrochloride inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) hydrochloride shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) hydrochloride shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10−6 cm/s[1].

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

Animal Model: CT-26 xenograft mice[1]
Dosage: 10 and 40 mg/kg
Administration: Oral adminstration (p.o.)
Result: Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
Animal Model: Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
Dosage: 10 mg/kg (p.o.), 2 mg/kg (i.v.)
Administration: Oral adminstration (p.o.) or intravenous injection (i.v.)
Result: Pharmacokinetic profile of CDK8-IN-11 (compound 29).
dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) F (%)
10 (p.o.) 1.1 0.8 453 31.7
2 (i.v.) 0.5 318
分子量

424.80

Formula

C19H16ClF3N4O2
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-11 hydrochloride 相关分类

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  • 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-11CDKβ-cateninCyclin dependent kinaseBeta cateninColorectalcolon cancerHCT-116CT-26WNTInhibitorinhibitorinhibit

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