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YKL-5-124

Chemical Structure : YKL-5-124

CAS No.: 1957203-01-8

YKL-5-124 (CDK7 inhibitor)

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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 515.618
Formula C28H33N7O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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

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