ATM Inhibitor SYH2051

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of ataxia telangiectasia mutated (ATM) kinase, with potential chemo-and radio-sensitizing and antineoplastic activities. Upon oral administration, ATM inhibitor SYH2051 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. SYH2051 hypersensitizes tumors to chemo/radiotherapy. 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.

**Synonyms:** - ATM KInase Inhibitor SYH2051 - SYH 2051 - SYH-2051 - SYH2051