1665195-94-7 Usage
Description
BAZ2A/B are bromodomain-containing proteins whose biological function, while not yet confirmed, is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci. A rare allele of BAZ2B has been identified to be a predictor of Sudden Cardiac Death. BAZ2-ICR is a small molecule inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains. It demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR has been shown to displace BAZ2 bromodomains in living cells by demonstrating accelerated FRAP recovery at 1 μM in the BAZ2A FRAP assay. See the Structural Genomics Consortium (SGC) website for more information.
Uses
BAZ2-ICR is a selective BAZ2 bromodomain inhibitor (IC50 values are 130 and 180 nM for BAZ2A and BAZ2B respectively). Exhibits 15-fold selectivity for the BAZ2 bromodomain over the CERC2 bromodomain and >100-fold selectivity over a range of other bromodomains. Accelerates FRAP recovery in a BAZ2A FRAP assay.
Check Digit Verification of cas no
The CAS Registry Mumber 1665195-94-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,6,6,5,1,9 and 5 respectively; the second part has 2 digits, 9 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1665195-94:
(9*1)+(8*6)+(7*6)+(6*5)+(5*1)+(4*9)+(3*5)+(2*9)+(1*4)=207
207 % 10 = 7
So 1665195-94-7 is a valid CAS Registry Number.
1665195-94-7Relevant articles and documents
Structure enabled design of BaZ2-ICR, a chemical probe targeting the bromodomains of BaZ2a and BaZ2B
Drouin, Ludovic,McGrath, Sally,Vidler, Lewis R.,Chaikuad, Apirat,Monteiro, Octovia,Tallant, Cynthia,Philpott, Martin,Rogers, Catherine,Fedorov, Oleg,Liu, Manjuan,Akhtar, Wasim,Hayes, Angela,Raynaud, Florence,Müller, Susanne,Knapp, Stefan,Hoelder, Swen
, p. 2553 - 2559 (2015)
The bromodomain containing proteins BaZ2a/B play essential roles in chromatin remodeling and regulation of noncoding RNas. We present the structure based discovery of a potent, selective, and cell active inhibitor 13 (BaZ2-ICR) of the BaZ2a/B bromodomains through rapid optimization of a weakly potent starting point. a key feature of the presented inhibitors is an intramolecular aromatic stacking interaction that efficiently occupies the shallow bromodomain pockets. 13 represents an excellent chemical probe for functional studies of the BaZ2 bromodomains in vitro and in vivo.
