CDK8-IN-12_product_DataBase

Bioactivity	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].
Invitro	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]。 Western Blot Analysis[1] Cell Line:
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]。
Name	CDK8-IN-12
CAS	2613307-67-6
Formula	C21H20ClN3O2
Molar Mass	381.86
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Mingfeng Yu, et al. Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. Eur J Med Chem. 2021 Mar 15;214:113248.

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