Preferred Label : ALC1 Inhibitor EIS-12656;
NCIt definition : An orally bioavailable allosteric inhibitor of the chromatin remodeling enzyme chromodomain-helicase-DNA-binding
protein 1-like (CHD1L; amplified in liver cancer 1; ALC1), with potential antineoplastic
activity. Upon oral administration, ALC1 inhibitor EIS-12656 selectively targets,
allosterically binds to and inhibits the activity of ALC1, thereby preventing ALC1/poly(ADP-ribose)
polymerase (PARP)-mediated repair of DNA breaks in tumor cells. This enhances the
accumulation of DNA strand breaks and promotes genomic instability eventually leading
to apoptosis. This inhibits tumor cell proliferation and may enhance the cytotoxicity
of PARP inhibitors and DNA-damaging agents. ALC1, a SNF2 family ATPase that modulates
the DNA retention of PARPs and other DNA repair enzymes, plays an important role in
DNA damage repair. It is overexpressed in cancer cells with homologous recombination
deficient (HRD) mutations. EIS-12656 is able to cross the blood-brain barrier (BBB).;
Molecule name : EIS-12656; EIS 12656;
Origin ID : C208256;
concept_is_in_subset
- has_target
