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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.