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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $79 | In Stock | |
5 mg | $188 | In Stock | |
10 mg | $279 | In Stock | |
25 mg | $479 | In Stock | |
50 mg | $686 | In Stock | |
100 mg | $997 | In Stock | |
1 mL x 10 mM (in DMSO) | $197 | In Stock |
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] |
Molecular Weight | 381.86 |
Formula | C21H20ClN3O2 |
Cas No. | 2613307-67-6 |
Storage | Powder: -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
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