|Solubility:||DMSO up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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.
How to Use:
- In vitro: PFI-3 was used at 1-10 µM final concentration in various in vitro assays.
- In vivo: n/a
- 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.
- Structural Genomics Consortium http://www.thesgc.org/chemical-probes
Products are for research use only. Not for human use.
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