A modulator of IRE1α function; binds to the ATP-binding site on IRE1α

APY-29 – 10 mg

Brand:
Cayman
CAS:
1216665-49-4
Storage:
-20
UN-No:
Non-Hazardous - /

APY-29 is a modulator of inositol requiring enzyme 1 α (IRE1α), which is a protein located in the endoplasmic reticulum (ER) membrane that has kinase and RNase activities triggered by ER stress.{36117} It binds to the ATP-binding site on IRE1α, where it inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM). In vitro, it restores the ability of dephosphoylated IRE1α to cleave XBP1 mRNA in a dose-dependent manner. It also enhances IRE1α oligomerization in a crosslinking assay.  

 

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SKU: 22913 - 10 mg Category:

Description

A modulator of IRE1α function; binds to the ATP-binding site on IRE1α, where it inhibits autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM); restores the ability of dephosphoylated IRE1α to cleave XBP1 mRNA in a dose-dependent manner; enhances IRE1α oligomerization in a crosslinking assay,

Formal name: N2-1H-benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine

Synonyms: 

Molecular weight: 332.4

CAS: 1216665-49-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Activators||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking

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