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
Molecular Formula
C48H52Cl2FN7O6
Molecular Weight
912.874
Shipping Conditions
Cool pack
Storage Temperature
-20°C
Available Sizes
Curated Selection
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