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CDK8-IN-12

Names

[ CAS No. ]:
2613307-67-6

[ Name ]:
CDK8-IN-12

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3
Signaling Pathways >> Epigenetics >> PKC
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3
Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

CDK8:14 nM (Ki)

GSK-3α:13 nM (Ki)

GSK-3β:4 nM (Ki)

PKCθ:109 nM (Ki)


[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]。 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.

[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]。

[References]

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C21H20ClN3O2

[ Molecular Weight ]:
381.86

Related Compounds