1403764-72-6 Usage
Description
PFI-1 is a selective BET bromodomain inhibitor that targets BRD2 and BRD4, playing a crucial role in regulating the expression of various growth-promoting and anti-apoptotic genes. It exhibits inhibitory activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM), and is known to induce apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines, such as MV4;11. Additionally, PFI-1 has been shown to downregulate Aurora B expression in these cells.
Uses
Used in Pharmaceutical Industry:
PFI-1 is used as a selective protein interaction inhibitor for targeting BET bromodomains, which are regulators required for the efficient expression of several growth-promoting and anti-apoptotic genes. This makes PFI-1 a potential therapeutic agent in the development of treatments for various diseases, particularly those involving uncontrolled cell growth or resistance to apoptosis.
Used in Cancer Research:
In cancer research, PFI-1 is used as a tool to study the role of BET bromodomains in the regulation of gene expression and their contribution to cancer progression. By inhibiting these bromodomains, PFI-1 can help researchers understand the underlying mechanisms of cancer development and identify potential therapeutic targets for cancer treatment.
Used in Drug Development:
PFI-1 is used as a lead compound in the development of new drugs targeting BET bromodomains. Its selective inhibition of BRD2 and BRD4 makes it a valuable starting point for designing more potent and specific inhibitors that can be used in the treatment of various diseases, including cancer.
Used in Cell Biology Research:
In cell biology research, PFI-1 is used to investigate the role of BET bromodomains in cell cycle regulation, apoptosis, and other cellular processes. By studying the effects of PFI-1 on cell lines like MV4;11, researchers can gain insights into the molecular mechanisms governing cell growth, division, and death, which can ultimately contribute to the development of novel therapeutic strategies.
Check Digit Verification of cas no
The CAS Registry Mumber 1403764-72-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,0,3,7,6 and 4 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1403764-72:
(9*1)+(8*4)+(7*0)+(6*3)+(5*7)+(4*6)+(3*4)+(2*7)+(1*2)=146
146 % 10 = 6
So 1403764-72-6 is a valid CAS Registry Number.
1403764-72-6Relevant articles and documents
NOVEL HETEROCYCLIC COMPOUNDS AS BROMODOMAIN INHIBITORS
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, (2013/03/26)
Disclosed are compounds of Formula (I): (I) which are useful as bromodomain inhibitors. Pharmaceutical compositions containing compounds of Formula (I) and the use of compounds of Formula (I) to treat diseases or disorders that are bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.
