CPI-455 (C09-1119-890)

CPI-455 is a specific, pan- KDM5 inhibitor with an IC 50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agentsIn VitroCPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. ?/nCPI-455, with high measured affinity for the target KDM5 proteins. Within 24 hours, increases in H3K4me3, are observed after exposure to either of the two active compounds, CPI-455 and CPI-766, in a dosedependent manner. IC 50 calculation for KDM5 Inhibitor CPI0455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoDual blockade of B7-H4 and KDM5B (CPI-455, 50/70 mg/kg, ip, daily) in mice elicits protective immunity. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-week-old male C57BL/6 mice (One- to 2-mm fragments of P. gingivalis –positive PDXs were implanted subcutaneously into the flank region of humanized mice.) Dosage: 50 mg/kg or 70 mg/kg (combined with anti–B7-H4). Administration: IP, daily, 14-28 days. Result: Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge. Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.Form:SolidIC50& Target:KDM5. Specification: 0.98 Molecular Formula: C16H14N4O Molecular Weight: 278.31 PubChem CID: 78426698 Isomeric SMILES: CC(C)C1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3