OF-1 - BRPF Bromodomain Inhibitor. CAS# 919973-83-4 Catalog No.:M60222-10S 4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine

4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine

Liesveld JL

pii: e8163

The selectivity of protein kinase inhibitors: a further update

CAS Number: 1620401-82-2

OF-1 - BRPF Bromodomain Inhibitor. CAS# 919973-83-4 Catalog No.:M60222-10S 4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amineOF 1, CAS No. 919973 83 4, is the potent and selective BRPF (BRomodomain and PHD Finger containing) inhibitor. It binds to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2. 4 mM (ITC). It has general >100 fold selectivity against other bromodomains (39 fold selectivity over BRD4). OF 1 increases thermal stability in the cellular thermal shift assay (CETSA) of full length BRPF1B at 1 M and also