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Chemical Structure : YKL-5-124
CAS No.: 1957203-01-8
Catalog No.: PC-36145Not For Human Use, Lab Use Only.
YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $488 | In stock | |
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| 100 mg | Get quote |
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YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM.
YKL-5-124 displays biochemical and cellular selectivity for CDK7 over structurally related kinases CDK12/13, and no significant activity against CDK2 and CDK9 (IC50>1 uM).
YKL-5-124 targets and forms a covalent bond with CDK7- cysteine 312 (C312).
Inhibition of CDK7 by YKL-5-124 elicits a transcriptional signature distinct from that of THZ1, shows no discernible effect on RNA Pol II CTD phosphorylation.
YKL-5-124 recapitulate THZ1-mediated effects on gene expression and CTD phosphorylation when combined with CDK12/13 inhibitor THZ531.
| M.Wt | 515.618 | |
| Formula | C28H33N7O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-3-(4-acrylamidobenzamido)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide |
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1. Olson CM, et al. Cell Chem Biol. 2019 Mar 6. pii: S2451-9456(19)30067-4.
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