[CAS NO. 1610358-56-9]  BAY 1251152

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PRODUCTS SPECIFICATIONS [1610358-56-9]

Store
Catalog
SLK-S8730
Brand
Selleck
CAS
1610358-56-9

DESCRIPTION [1610358-56-9]

Overview

MDL-
Molecular Weight404.43
Molecular FormulaC19H18F2N4O2S
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.4726 mL12.3631 mL24.7262 mL
5 mM0.4945 mL2.4726 mL4.9452 mL
10 mM0.2473 mL1.2363 mL2.4726 mL
50 mM0.0495 mL0.2473 mL0.4945 mL

Description

BAY1251152 is a potent inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.

Targets

CDK9 [2]
(Cell-free assay)
3 nM

In vitro

BAY 1251152 (compound 2) significantly inhibits CDK9 and CDK2 with IC50 of 3 nM and 360 nM, respectively. BAY 1251152 (compound 2) shows cellular potency in MOLM13 with IC50 of 29 nM.