An orally bioavailable inhibitor of p97 (IC50 = 11 nM); causes accumulation of poly-ubiquitinated proteins

CB-5083 – 25 mg

Brand:
Cayman
CAS:
1542705-92-9
Storage:
-20
UN-No:
Non-Hazardous - /

CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP).{32505,32506} It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.{32505,32506}  

 

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Description

An orally bioavailable inhibitor of p97 (IC50 = 11 nM); causes accumulation of poly-ubiquitinated proteins, retention of ERAD substrates, and activation of the apoptotic arm of the unfolded protein response

Formal name: 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide

Synonyms: 

Molecular weight: 413.5

CAS: 1542705-92-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|ER Protein Folding||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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