RGNCY-0051 (DDRI-9 DNA damage response inhibitor)
DDRI-9 is a DNA damage response inhibitor that inhibits phosphorylated histone variant H2AX foci formation upon DNA damage. It also enhances the cytotoxicity of etoposide and ionizing radiation. DDRI-9 reduces the foci formation of DNA repair-related proteins including the protein kinase ataxia-telangiectasia mutated, DNA-dependent protein kinase, breast cancer type 1 susceptibility protein and p53-binding protein 1 but not the mediator of DNA damage checkpoint protein 1. DDRI-9 blocks mitotic progression and the accumulation of mitotic protein and induces cell death by apoptosis. This suggests that DDRI-9 may be a lead molecule for the development of more enhanced anti-cancer drugs.
Systematic Name: N-(7-(4-fluorobenzyl)-3-methyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)methanimine oxide
Mol Wt: 317.28
Tags: Apoptosis, DNA damage, RGNCY-0051, DDR1-9, DDR1