KT-253

• 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

• Molecular Formula:

  C48H52Cl2FN7O6

• Molecular Weight:

  912.874

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2713618-08-5