CDK2/CDK4 Degrader NKT5097

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable dual protein degrader of cyclin-dependent kinase (CDK) types 2 (CDK2) and 4 (CDK4), with potential antineoplastic activity. Upon oral administration, CDK2/CDK4 degrader NKT5097 targets, binds to and degrades CDK2 and CDK4, which inhibits the cyclin E1 (CCNE1)/CDK2 and cyclin D1/CDK4 cell cycle pathways. This inhibits the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase and prevents CDK-mediated G1-S-phase transition, which leads to cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. CDKs are serine/threonine kinases that are important regulators of cell cycle progression and cellular proliferation and are upregulated in many tumor cell types. Cyclin E1 and cyclin D1 are also overexpressed in various tumor cell types.

**Synonyms:** - CDK2/4 Degrader NKT5097 - CDK2/CDK4 Dual Degrader NKT5097 - NKT 5097 - NKT-5097 - NKT5097