Toggle Nav
Close
  • Menu
  • Setting

PFI 3

Catalog No.
B7744
inhibitor of polybromo 1 and SMARCA4
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
10mg
$130.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PFI 3 is a potent and selective inhibitor of polybromo 1 and SMARCA4 with Kd values of 48 and 89 nM, respectively [1].

Transcription activator BRG1 (SMARCA4) is a member of the SWI/SNF family and regulates transcription. Protein polybromo-1 (PB1, PBRM1) is a BRG1-associated factor and tumor suppressor.

PFI 3 is a potent and selective inhibitor of polybromo 1 and SMARCA4. PFI 3 bound to SMARCA2 and SMARCA4 bromodomains with Kd values of 55 and 110 nM, respectively. PFI-3 (2 μM) inhibited PBRM1 by 70%. In cell-based chromatin binding assays, PFI-3 replaced GFP-tagged SMARCA2 bromodomain in a dose-dependent way with IC50 value of 5.78 μM. PFI-3 was a cell-permeable probe suitable for studying SMARCA2/4 bromodomains. In the SMARCA4-deficient A549, H1299, H157 cell lines, PFI-3 had no anti-proliferative effects and was unable to replace SMARCA2 from chromatin. In THP-1 and MV4-11 leukemic cells, PFI 3 did not induce anti-cancer phenotype [1].

Reference:
[1].  Vangamudi B, Paul TA, Shah PK, et al. 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. Cancer Res, 2015, pii: canres.3798.2015.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt321.37
Cas No.1819363-80-8
FormulaC19H19N3O2
Solubilityinsoluble in H2O; ≥15.15 mg/mL in DMSO; ≥2.97 mg/mL in EtOH with ultrasonic
SDFDownload SDF
Canonical SMILESO=C(C1=CC=CC=C1O)/C=C/N(C2)[[email protected]@H]3C[[email protected]]2N(C4=NC=CC=C4)C3
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

PFI 3