CPI-455 HCl (C09-0823-249)

InformationCPI-455 HCl CPI-455 is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.TargetsKDM5A (Cell-free assay) 10 nMIn vitroCPI-455 has improved potency against KDM5A while demonstrating ~200-fold selectivity for KDM5A over KDM4C. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no measurable inhibition of KDM2B, KDM3B or KDM6A. CPI-455-mediated KDM5 inhibition results in a dose-dependent increase in global H3K4me3 in HeLa cells. CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site.Cell Research(from reference)Cell lines：melanoma (M14), breast cancer (SKBR3) and NSCLC (PC9) cell lines Concentrations：0-25 μM Incubation Time：14-20 days. Specifications and Purity: 99%. Molecular Formula: C16H15ClN4O. Molecular Weight: 314.77. PubChem CID: 129896721. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/C413962-SCI_b76133667e2e7cbbc08104018f2df3b0.pdf.