Preferred Label : PKMYT1 Inhibitor XL495;
NCIt definition : An orally bioavailable small molecule inhibitor of the human membrane-associated tyrosine-
and threonine-specific cdc2-inhibitory kinase (PKMYT1), with potential antineoplastic
activity. Upon oral administration, PKMYT1 inhibitor XL495 targets, binds to and inhibits
the activity of PKMYT1. This results in the inhibition of CDK1 phosphorylation, which
may promote both premature mitosis and a prolonged mitotic arrest, and lead to the
accumulation of unrepaired DNA damage and apoptosis in susceptible tumor cells, such
as CCNE1-overexpressing tumor cells. PKMYT1 phosphorylates CDK1 specifically when
CDK1 is complexed to cyclins, which blocks progression from G2 into mitosis.;
Molecule name : XL-495; XL 495;
Origin ID : C213585;
concept_is_in_subset
- has_target
