PARP1 Inhibitor EIK1004

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable, central nervous system (CNS)-active inhibitor of nuclear enzyme poly(ADP-ribose) polymerase (PARP) 1, with potential antineoplastic activity. Upon oral administration, PARP1 inhibitor EIK1004 selectively binds to and inhibits the activity of PARP1, thereby preventing the repair of damaged DNA via the base excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks and promotes genomic instability eventually leading to apoptosis. PARP1 catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and plays a key role in the repair of single strand DNA (ssDNA) breaks and double-strand breaks (DSBs). EIK1004 is able to cross the blood-brain barrier (BBB). As a PARP1 selective inhibitor, EIK1004 does not induce PARP2-related hematologic suppression as is seen with nonselective PARP inhibitors.

**Synonyms:** - EIK 1004 - EIK-1004 - EIK1004 - IMP 1707 - IMP-1707 - IMP1707 - PARP1 Inhibitor IMP1707 - PARP1 Selective Inhibitor EIK1004