PFI-3 --- SMARCA Bromodomains Inhibitor
Overview | |
Catalog # | bs-60175c-2-mg-solid |
Product Name | PFI-3 --- SMARCA Bromodomains Inhibitor |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 321.37 Formula: C19 H19 N3 O2 CAS Number: 1819363-80-8 InChi Key: INAICWLVUAKEPB-QSTFCLMHSA-N InChi: InChI=1S/C19H19N3O2/c23-17-6-2-1-5-16(17)18(24)8-10-21-12-15-11-14(21)13-22(15)19-7-3-4-9-20-19/h1-10,14-15,23H,11-13H2/b10-8+/t14-,15-/m1/s1 Smiles: OC1C=CC=CC=1C(=O)/C=C/N1C[C@H]2C[C@@H]1CN2C1C=CC=CN=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | PFI-3 is a novel potent, selective and cell permeable inhibitor of SMARCA4 and PB1(5) bromodomains with IC50 ~ 89 nM and 48 nM respectively. It also inhibits SMARCA2, but has no interaction with the other sub-family branches including PB1(2-4) and a kinase panel of 36 kinases. It accelerates FRAP recovery in cells at a concentration of 1 μM. The SWI/SNF-related, Matrix-associated, Actin-dependent Regulator of Chromatin (SMARC) proteins integrate into complexes that remodel chromatin. The SMARC family A (SMARCA) members SMARCA2 (also known as BRM) and SMARCA4 (also known as BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins. PFI-3 is a very useful chemical probe to study the key chromatin remodeling and transcription control. |