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Chemical Structure : LY2857785
CAS No.: 1619903-54-6
Catalog No.: PC-42956Not For Human Use, Lab Use Only.
LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CDK7 (IC50=246 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $238 | In stock | |
| 25 mg | $398 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CDK7 (IC50=246 nM).
LY2857785 showes good selectivity against a panel of 114 protein kinases.
LY2857785 inhibits RNAP II C-terminal domain (CTD) P-Ser2 and CTD P-Ser5 in U2OS cells with IC50 of 89 and 42 nM, dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines (MV-4-11 cell IC50=40 nM).
LY2857785 inhibits RNAP II CTD P-Ser2 in vivo, demonstrates potent antitumor growth efficacy in tumor xenografts.
| M.Wt | 448.6036 | |
| Formula | C26H36N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1,4-Cyclohexanediamine, N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-, trans- |
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1. Yin T, et al. Mol Cancer Ther. 2014 Jun;13(6):1442-56.
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