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PFI 1

Catalog #: 4445
4 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4445/10
4445/50
PFI 1 | CAS No. 1403764-72-6 | Bromodomain Inhibitors
1 Image
Description: BET bromodomain inhibitor

Chemical Name: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide

Purity: ≥98%

Product Details
Citations (4)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

PFI 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 Information

Chemicalprobes.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.

Technical Data

M.Wt:
347.39
Formula:
C16H17N3O4S
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at RT
CAS No:
1403764-72-6

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.

Additional Information

Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 1 probe summary on the SGC website.

Product Datasheets

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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

  1. 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
  2. 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
  3. 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
  4. 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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