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IRE1α kinase-IN-1

Catalog No. T9564 CAS 2328097-41-0

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

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IRE1α kinase-IN-1, CAS 2328097-41-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 147.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 556.00
25 mg	In stock	$ 896.00
50 mg	In stock	$ 1,220.00
100 mg	In stock	$ 1,650.00
1 mL * 10 mM (in DMSO)	In stock	$ 397.00

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Purity: 99.18%

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Description

In vitro

IRE1α kinase-IN-1 (compound 31) effectively mitigates endoplasmic reticulum stress by hindering IRE1α oligomerization and phosphorylation, while also suppressing its endoribonuclease activity within human cells[1]. Demonstrating exceptional specificity, this compound shows greater than 70% inhibition for only 4 out of 455 kinases tested, highlighting its select focus on IRE1α. It notably attenuates recombinant G547 IRE1α KEN domain pS274 autophosphorylation, achieving an IC50 of 160 nM, and disrupts ATP-site LanthaScreen tracer binding to the recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1]. Additionally, it prevents tunicamycin-induced GFP-IRE1α foci formation in HEK293 cells with an IC50 value of 0.74 μM and obstructs both tunicamycin- and thapsigargin-induced IRE1α-dependent XBP1 mRNA splicing, with IC50 values ranging from 0.68 to 1.63 μM in the same cell line[1]. Moreover, in H929 and NCI-H929 cells, IRE1α kinase-IN-1 dose-dependently suppresses IRE1α-dependent XBP1s mRNA expression when applied at concentrations between 0 to 20 μM, demonstrating its potent inhibitory activity on tunicamycin-induced XBP1s expression[1].

Molecular Weight	504.99
Formula	C26H26ClFN8
CAS No.	2328097-41-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (19.8 mM), Sonication is recommended.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

MKC9989 Sunitinib GSK2850163 (S enantiomer) IRE1α kinase-IN-8 B I09 IXA6 STF-083010 Kira8

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Keywords

IRE1α kinase-IN-1 2328097-41-0 Cell Cycle/Checkpoint IRE1 endoribonuclease Inositol requiring enzyme 1 cells IRE1a kinase-IN-1 oligomerization IRE-1α kinase-IN-1 selectivity IRE1α kinase IN 1 Inhibitor inhibit IRE1alpha kinase-IN-1 HEK293 autophosphorylation reticulum IRE1α kinaseIN1 endoplasmic inhibitor

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