纯度:98% by HPLC;NMR (Conforms)
分子式:C16H14N4O
分子量:278.32
溶剂:DMSO (>25 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):Lysine demethylase KDM5 inhibitor
Function / Pharmacology: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