BS-181
BS-181 is a potent, selective CDK7 inhibitor with IC50 of 21 nM, 40-fold selectivity over CDK2/cycE and no significant activity against CDK1/cycB, CDK4/cycD1, CDK5/p35NCK, CDK6/cycD1, and CDK9/cycT (IC50>1 uM) ; promotes cell cycle arrest and inhibits cancer cell growth in a panel of cell lines representing a range of tumor types (IC50=1.5 to 37 uM), inhibits the phosphorylation of CDK7 substrates, inhibits phosphorylation of the RNA polymerase II COOH-terminal domain (CTD) at P-Ser5 (IC50=9 uM), inhibits RB phosphorylation at Ser795 and Ser821 (IC50=15 uM) ; induces apoptosis in vitro, and shows antitumor effects in vivo.
Product Specifications
CAS Number
1092443-52-1
Product Name Alternative
BS 181 | BS181
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
CC (C) C1=C2N=C (NCCCCCCN) C=C (NCC3=CC=CC=C3) N2N=C1
Molecular Formula
C22H32N6
Molecular Weight
380.53
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5- (6-aminohexyl) -3- (1-methylethyl) -N7- (phenylmethyl) -
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