PFI-1

PFI-1, a chemical probe, is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.

Product Specifications

CAS Number

[1403764-72-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pfi-1.html

Purity

99.87

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O

Molecular Formula

C16H17N3O4S

Molecular Weight

347.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Picaud S, et al. PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains. Cancer Res. 2013 May 21. [Epub ahead of print]|[2]Fish PV, et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem. 2012 Nov 26;55 (22) :9831-7.|[3]Cheng Z, et al. Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clin Cancer Res. 2013 Apr 1;19 (7) :1748-59.|[4]Kate E Lines, et al. Epigenetic modifiers reduce proliferation of human neuroendocrine tumour cell lines. Endocrine Abstracts (2013) 31 P149