GSK5959 --- BRPF1 Bromodomain Inhibitor

Overview
Catalog #	bs-60239c-2-mg-solid
Product Name	GSK5959 --- BRPF1 Bromodomain Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 394.47 Formula: C22 H26 N4 O3 CAS Number: 901245-65-6 InChi Key: LTUGYAOMCKNTGG-UHFFFAOYSA-N InChi: InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27) Smiles: COC1C=CC=CC=1C(=O)NC1=CC2=C(C=C1N1CCCCC1)N(C)C(=O)N2C Purity: 98.0 Solubility: DMSO up to 10 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	GSK5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. It has >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. A cellular protein interaction assay measuring the displacement of NanoLuc-tagged BRPF1 bromodomain from Halotagged histone H3.3 was employed to demonstrate GSK5959’s cell permeability and disruption of chromatin binding with IC50 ~0.98 µM.