IRE1α kinase-IN-1

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) [1].

Product Specifications

CAS Number

[2328097-41-0]

UNSPSC

12352005

Hazard Statement

H301, H311, H331

Target

IRE1

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ire1α-kinase-in-1.html

Purity

98.94

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CN1CCC(CNC2=CC(Cl)=NN3C2=NC=C3C4=C(F)C=C5C(N=C(NC6=CC=CC=C6)N5)=C4)CC1

Molecular Formula

C26H26ClFN8

Molecular Weight

504.99

Precautions

H301, H311, H331

References & Citations

[1]Colombano G, et al. Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease. J Med Chem. 2019;62 (5) :2447-2465.