CDK8-IN-12

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].

Product Specifications

CAS Number

[2613307-67-6]

UNSPSC

12352005

Target

CDK; GSK-3; PKC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cdk8-in-12.html

Purity

99.74

Solubility

DMSO : 66.67 mg/mL (ultrasonic)

Smiles

O=C1NCCC12CCN(C3=C(C4=CC5=CC=CC=C5O4)C=NC=C3Cl)CC2

Molecular Formula

C21H20ClN3O2

Molecular Weight

381.86

References & Citations

[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.