Chemical Name: 7-Oxo-5-phenyl-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
Lysine demethylase KDM5 inhibitor
Molekulargewicht:
278.32
Reinheit:
98% by HPLC NMR (conforms)
Formulierung:
Off-white solid
CAS Nummer:
[1628208-23-0]
Formel:
C16H14N4O
Anwendungsbeschreibung:
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).1 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.2 KDM5 demethylases have recently been shown to repress the immune response to tumors via suppression of STING.3
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