PFI-3

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 (BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins. The protein polybromo-1 (PB1, BRG1-associated factor) contains six bromodomains, but only the fifth (PB1(5)) shares the same structural signature as those of SMARCA2 and SMARCA4. PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. Evaluation of interactions of PFI-3 with different classes of bromodomains using thermal stability assay indicates that PFI-3 interacts selectively with bromodomains from SMARCA2 and SMARCA4 as well as the fifth domain of PB1. Similarly, PFI-1 (Cay-11155) does not interact with a panel of kinases. See the Structural Genomics Consortium (SGC) website for more information.Formal Name: (2E)-1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-2-propen-1-one. CAS Number: 1819363-80-8. Molecular Formula: C19H19N3O2. Formula Weight: 321.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.15 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 211, 230, 247, 362 nm. SMILES: OC1=C(C(/C=C/N2[C@H](C3)CN(C4=NC=CC=C4)[C@H]3C2)=O)C=CC=C1. InChi Code: 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. InChi Key: INAICWLVUAKEPB-QSTFCLMHSA-N.