YKL-5-124 | CDK7 inhibitor | Probechem Biochemicals

Chemical Structure : YKL-5-124

CAS No.: 1957203-01-8

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YKL-5-124 (CDK7 inhibitor)

货号: 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.

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5 mg	￥1880	In stock
10 mg	￥2980	In stock
25 mg	￥4880	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	515.618
分子式	C28H33N7O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

1. Olson CM, et al. Cell Chem Biol. 2019 Mar 6. pii: S2451-9456(19)30067-4.

YKL-5-124 (CDK7 inhibitor)

生物&药学活性

物理化学性质&存储条件

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YKL-5-124 (CDK7 inhibitor)

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物理化学性质&存储条件

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