Chemical Name: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
Biological ActivityPFI 1 is a potent BET bromodomain inhibitor; exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4 (IC50 values are 98 and 220 nM respectively). Induces apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). Also downregulates Aurora B expression in MV4;11 cells. Cell permeable.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PFI 1 is reviewed on the chemical probes website.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish et al.
J.Med.Chem. [Epub ahead of print], 2012;
Citations for PFI 1
The citations listed below are publications that use Tocris products. Selected citations for PFI 1 include:
4 Citations: Showing 1 - 4
Epigenetic inactivation of the 5-methylcytosine RNA methyltransferase NSUN7 is associated with clinical outcome and therapeutic vulnerability in liver cancer.
Authors: Fernando Et al.
Mol Cancer 2023;22:83
Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL.
Authors: Christopher J Et al.
Cancer Res 2022;82:3375-3393
CXCL8 histone H3 acetylation is dysfunctional in airway smooth muscle in asthma: regulation by BET.
Authors: Clifford Et al.
Am J Physiol Lung Cell Mol Physiol 2015;308:L962
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Authors: Fish Et al.
J Med Chem 2012;55:9831
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