KT-253

Product Specifications

CAS Number

2713618-08-5

Target

MDM-2/p53|||Apoptosis|||PROTACs

Related Pathways

Apoptosis|||PROTAC

Bioactivity

KT-253 is a p53 stabilizer and a PROTAC degrader of MDM2 (DC50=0.4 nM) . It inhibits the proliferation of cancer cells RS4;11 with an IC50 of 0.3 nM, induces cell cycle arrest in the G2/M phase, and triggers apoptosis. In mouse models, KT-253 demonstrates antitumor activity. (Pink: ligand for target protein MDM2 ligand 4; Black: linker; Blue: ligand for E3 ligase cereblon)

Smiles

O=C1[C@@]2(C3(N[C@@H](C(N[C@@H]4CC[C@@H](C(=O)N5CCC(CC5)C=6C=C7C(=CC6)N(C(=O)N7C)C8C(=O)NC(=O)CC8)CC4)=O)[C@@H]2C9=C(F)C(Cl)=CC=C9)CCCCC3)C=%10C(N1)=CC(Cl)=CC%10