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.
CAS Number: 1819363-80-8
Molecular Weight: 321.37
Chemical Name: (E)-1-(2-hydroxyphenyl)-3-((1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)prop-2-en-1-one
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PFI-3 was used at 1-10 µM final concentration in various in vitro assays.
- Witkowski L, et al. Germline and somatic SMARCA4 mutations characterize small cell carcinoma of the ovary, hypercalcemic type. (2014) Nat Genet. In press.
- Ramos P, et al. Small cell carcinoma of the ovary, hypercalcemic type, displays frequent inactivating germline and somatic mutations in SMARCA4. (2014) Nat Genet. In press.
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