2. PROTAC Apoptosis
  3. PROTACs MDM-2/p53 Apoptosis
  4. KT-253

KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. KT-253 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))

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KT-253 Chemical Structure

KT-253 Chemical Structure

CAS No. : 2713618-08-5

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KT-253 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. KT-253 exhibits antitumor efficacy in mouse models[1]. (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))

Molecular Weight

912.87

Formula

C48H52Cl2FN7O6
CAS No.
SMILES

ClC1=CC2=C([C@]3(C4(CCCCC4)N[C@@H](C(N[C@H]5CC[C@H](C(N6CCC(C7=CC=C8C(N(C)C(N8C9CCC(NC9=O)=O)=O)=C7)CC6)=O)CC5)=O)[C@@H]3C%10=C(F)C(Cl)=CC=C%10)C(N2)=O)C=C1
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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KT-253 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KT-2532713618-08-5KT253KT 253PROTACsMDM-2/p53ApoptosisRS4;11MOLM-13NOG mouseAMLInhibitorinhibitorinhibit

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