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YKL-5-124 TFA

Product Specifications

CAS Number

2748220-93-9

Target

Others, CDK

Related Pathways

Others, Cell Cycle/Checkpoint

Bioactivity

YKL-5-124 TFA, a potent and selective irreversible covalent inhibitor of CDK7, demonstrates IC50 values of 53.5 nM for CDK7 and 9.7 nM for the CDK7/Mat1/CycH complex. It exhibits over 100-fold selectivity for CDK7 over CDK9 and CDK2, while showing no activity against CDK12 and CDK13. This compound effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on the phosphorylation status of RNA polymerase II.

Smiles

C(C(O)=O)(F)(F)F.N(C(=O)C1=CC=C(NC(C=C)=O)C=C1)C=2C3=C(C(C)(C)N(C(N[C@H](CN(C)C)C4=CC=CC=C4)=O)C3)NN2

Molecular Formula

C30H34F3N7O5

Molecular Weight

629.63

Shipping Conditions

Ice Packs

Storage Temperature

-20°C

Available Sizes

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