OF-1 --- BRPF Bromodomain Inhibitor

Overview
Catalog #	bs-60222c-2-mg-solid
Product Name	OF-1 --- BRPF Bromodomain Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 440.31 Formula: C17 H18 Br N3 O4 S CAS Number: 919973-83-4 InChi Key: YUNQZQREIHWDQT-UHFFFAOYSA-N InChi: InChI=1S/C17H18BrN3O4S/c1-10-7-11(18)5-6-16(10)26(23,24)19-12-8-13-14(9-15(12)25-4)21(3)17(22)20(13)2/h5-9,19H,1-4H3 Smiles: CC1C=C(Br)C=CC=1S(=O)(=O)NC1=CC2=C(C=C1OC)N(C)C(=O)N2C Purity: 98.0 Solubility: DMSO up to 20 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	OF-1 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 µM and also demonstrates accelerated FRAP recovery at 5 µM in the BRPF2 FRAP assay. It shows modest general cytotoxicity.