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CDK8-IN-12

CDK8-IN-12
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Purity:99.83%
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CDK8-IN-12

Catalog No. T72048Cas No. 2613307-67-6
CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.
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Pack SizePriceAvailabilityQuantity
1 mg$79In Stock
5 mg$188In Stock
10 mg$279In Stock
25 mg$479In Stock
50 mg$686In Stock
100 mg$997In Stock
1 mL x 10 mM (in DMSO)$197In Stock
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Product Introduction

Bioactivity
Description
CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.
Targets&IC50
CDK8:14 nM(Ki), MV-4-11 cells:0.36 μM(GI50), GSK-3α:13 nM(ki), GSK-3β:4 nM(ki), PCKθ:109 nM(ki)
In vitro
CDK8-IN-12 (0.36, 0.72 μM ; 2 h) significantly reduced the phosphorylation of STAT1 serine 727.[1]
In vivo
CDK8-IN-12 (intravenous administration ; 5 mg/kg in rats ; 2 mg/kg in mice) had a T1/2 of 0.9 h and 0.34 h in rats and mice, respectively.[1]
Chemical Properties
Molecular Weight381.86
FormulaC21H20ClN3O2
Cas No.2613307-67-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 27.5 mg/mL (72.02 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6188 mL13.0938 mL26.1876 mL130.9380 mL
5 mM0.5238 mL2.6188 mL5.2375 mL26.1876 mL
10 mM0.2619 mL1.3094 mL2.6188 mL13.0938 mL
20 mM0.1309 mL0.6547 mL1.3094 mL6.5469 mL
50 mM0.0524 mL0.2619 mL0.5238 mL2.6188 mL

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