An antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM); orally bioavailable

JNJ-26854165 – 5 mg

Brand:
Cayman
CAS:
881202-45-5
Storage:
-20
UN-No:
Non-Hazardous - /

The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.{26610,20554} JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).{27796} It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.{27796} JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.{20554} As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.{20554,27795,27797}  

 

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Description

An antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways

Formal name: N1-[2-(1H-indol-3-yl)ethyl]-N4-4-pyridinyl-1,4-benzenediamine

Synonyms:  Serdemetan

Molecular weight: 328.4

CAS: 881202-45-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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