CPI-455, Lysine demethylase KDM5 inhibitor (TBI4035)

Description

Product Details

Formal Name: 7-Oxo-5-phenyl-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile

Molecular Formula: C₁₆H₁₄N₄O

Formula Weight: 278.32

CAS Number: 1628208-23-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Lysine demethylase KDM5 inhibitor

Functions

CPI-455 (1628208-23-0) is a potent (IC50 = 10 nM) and selective inhibitor of the lysine demethylase KDM5 (equal inhibition of KDM5A, 5B, 5C). CPI-455 reduced the number of drug-tolerant persister cancer cells (DTPs) in a dose-dependent, KDM5-dependent manner in multiple cell lines treated with standard chemotherapy or targeted agents. CPI-455 synergized with 5-aza-2’-deoxycytidine (DAC) to reduce the viability of luminal breast cancer cells in vitro. KDM5 demethylases have recently been shown to repress the immune response to tumors via suppression of STING.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.