1. Cell Cycle/DNA Damage Stem Cell/Wnt Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. CDK Wnt β-catenin c-Myc Reactive Oxygen Species (ROS)
  3. CDK8-IN-20

CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC50 of 70.5 nM. CDK8-IN-20 shows IC50 values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer.

For research use only. We do not sell to patients.

CDK8-IN-20

CDK8-IN-20 Chemical Structure

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Description

CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC50 of 70.5 nM. CDK8-IN-20 shows IC50 values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer[1].

IC50 & Target[1]

CDK8

70.5 nM (IC50)

CDK19

147.8 nM (IC50)

CDK9

217.4 nM (IC50)

CDK7

726.9 nM (IC50)

In Vitro

CDK8-IN-20 can inhibit HCT-116, HT-29 and SW-480 cell proliferation with an IC50 values of 5.9, 17.93 and 9.52 μM and has low cytotoxicity for normal gastric mucosal epithelial cells GES-1 (IC50 > 100 μM)[1].

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

Molecular Weight

469.51

Formula

C22H23N5O5S

SMILES

O=C(C1=CC=CN1)NC2=CC(NS(=O)(C3=C(C)C=C(C(N4C)=C3)N(C)C4=O)=O)=CC(OC)=C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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CDK8-IN-20
Cat. No.:
HY-180124
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