Preferred Label : ATM Kinase Inhibitor WSD-0628;
NCIt synonyms : ATM Inhibitor WSD-0628;
NCIt related terms : WSD-0628;
NCIt definition : An orally bioavailable, brain-penetrable inhibitor of ataxia telangiectasia mutated
(ATM) kinase, with potential chemo-and radio-sensitizing and antineoplastic activities.
Upon oral administration, ATM kinase inhibitor WSD-0628 selectively targets and binds
to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling.
This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces
apoptosis in damaged tumor cells, and leads to cell death in ATM-overexpressing tumor
cells. WSD-0628 hypersensitizes tumors to chemo/radiotherapy. In addition, WSD-0628
is able to cross the blood-brain barrier (BBB). ATM, a serine/threonine protein kinase
belonging to the phosphatidylinositol 3-kinase-related kinase (PIKK) family of protein
kinases, is upregulated in a variety of cancer cell types. It is activated in response
to DNA double-strand breaks (DSB) and plays a key role in DNA repair.;
UNII : KTC2HLR3RE;
CAS number : 2765448-96-0;
Molecule name : WSD 0628; WSD-0628;
NCI Metathesaurus CUI : CL1920426;
Origin ID : C201515;
UMLS CUI : C5854654;
Semantic type(s)
- concept_is_in_subset
- has_target
