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.
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- 화학식: C22H23N5O5S
- 분자량:469.51
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
CDK8 70.5 nM (IC50) |
CDK19 147.8 nM (IC50) |
CDK9 217.4 nM (IC50) |
CDK7 726.9 nM (IC50) |
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.
Chemical Information
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분자량 469.51
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화학식 C22H23N5O5S
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)