PFI-1 is an inhibitor of BET bromodomains (BRDs) that prevents the association of BET with histones; it acts as an acyl-lysine (Kac) mimetic inhibitor, binding the Kac site of BRD2 and BRD4. PFI-1 exhibits anti-inflammatory and anticancer activities. In H202-treated bronchial epithelial cells, PFI-1 decreases expression of IL-6 and CXCL8. In leukemia cells, PFI-1 downregulates expression of Myc and AurKB, inducing G1 phase cell cycle arrest and suppressing cell growth.
| Cas No. | 1403764-72-6 |
|---|---|
| Purity | ≥98% |
| Formula | C16H17N3O4S |
| Formula Wt. | 347.39 |
| IUPAC Name | 2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide |
| Synonym | PF-06405761 |
| Solubility | DMSO 69 mg/mL (198.62 mM) Water Insoluble Ethanol Insoluble |
| Appearance | White to off white powder |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
|---|---|
| Info Sheet |
Khan YM, Kirkham P, Barnes PJ, et al. Brd4 Is Essential for IL-1β-Induced Inflammation in Human Airway Epithelial Cells. PLoS One. 2014 Apr 23;9(4):e95051. PMID: 24759736.
Picaud S, Da Costa D, Thanasopoulou A, et al. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res. 2013 Jun 1;73(11):3336-46. PMID: 23576556.
