nutlin-3a

Nutlin-3a is a **small molecule inhibitor** targeting the interaction between **MDM2** (Mouse double minute 2 homolog) and the tumor suppressor protein **p53**. By binding to MDM2, Nutlin-3a prevents the ubiquitination and proteasomal degradation of p53, resulting in its **stabilization and activation of p53 signaling pathways**. This activates p53-dependent processes such as cell cycle arrest, apoptosis, and senescence, particularly in cancers that retain wild-type p53 function. Nutlin-3a displays efficacy in preclinical models across various pediatric and adult cancers, including **retinoblastoma, rhabdomyosarcoma, neuroblastoma, lymphoma, leukemia, and sarcoma**. It is characterized as a **nongenotoxic agent** with lower toxicity compared to conventional therapies, and demonstrates additive or synergistic effects when used in combination with DNA-damaging agents such as cisplatin. Additional preclinical research has indicated that Nutlin-3a may inhibit the efflux function of breast cancer resistance protein (BCRP), potentially sensitizing cancer cells to different chemotherapies[1][2][3][4][5][6][8].

Brand names

Rebemadlin

Other names

Nutlin-3aNutlin3aNutlin 3a(-)-Nutlin-3Nutlin-3a chiralNutlin3a chiralNutlin 3a chiralCS-391CS391CS 391Nutlin-3a USP/EP/BPMDM2 Antagonist IVMDM-2 Antagonist IVMDM 2 Antagonist IVp53-MDM2 binding inhibitorp-53-MDM2 binding inhibitorp 53-MDM2 binding inhibitor