PFI-3

• CAT Number: I005862
• Molecular Formula: C19H19N3O2
• Molecular Weight: 321.37
• Purity: ≥95%
• Target: PBRM1/SMARCA4
• Solubility: Soluble to 100 mM in DMSO and to 100 mM in ethanol
• Storage: Store at -20°C
• IC50: 48 nM/89 nM(PBRM1/SMARCA4)

PFI-3 is a potent and selective polybromo 1 and SMARCA4 inhibitor (Kd values are 48 and 89 nM respectively).


PFI-3 also inhibits SMARCA2. PFI-3 displays 30-fold selectivity over other sub-family branches. PFI-3 accelerates FRAP recovery in cells at a concentration of 1 μM.

Reference

[1]The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.
Vangamudi B, Paul TA, Shah PK, Kost-Alimova M, Nottebaum L, Shi X, Zhan Y, Leo E, Mahadeshwar HS, Protopopov A, Futreal A, Tieu TN, Peoples M, Heffernan TP, Marszalek JR, Toniatti C, Petrocchi A, Verhelle D, Owen DR, Draetta G, Jones P, Palmer WS, Sharma S, Andersen JN.
Cancer Res. 2015 Sep 15;75(18):3865-78. doi: 10.1158/0008-5472.CAN-14-3798. Epub 2015 Jul 2.
PMID: 26139243