CDK8-IN-11 hydrochloride

价格：询价

品牌：MedChemExpress(MCE) 品牌认证

货号：HY-151463A

产品详情

CDK8-IN-11 hydrochloride

CAS No. :

MCE 国际站：CDK8-IN-11 hydrochloride

产品活性：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。

研究领域：Cell Cycle/DNA Damage | Stem Cell/Wnt

作用靶点：CDK | β-catenin

In Vitro: CDK8-IN-11 (compound 29, 200 nM) hydrochloride shows inhibitory effects against CDK8 by 73.6% .
CDK8-IN-11 (0-50 μM, 48 h) hydrochloride inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells.
CDK8-IN-11 (0-4 μM, 48 h) hydrochloride inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells.
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.
CDK8-IN-11 (0.5-2 μM, 48 h) hydrochloride increases the number of cells in the G1 phase in HCT-116 cells.
CDK8-IN-11 (0-4 μM) hydrochloride reverses Sorafenib (HY-10201) resistance of HCT-116 cells.

In Vivo: CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) hydrochloride inhibits tumor growth in CT-26 xenograft mice.
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) hydrochloride shows no obvious abnormal behavior within 7 days.
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.