532281 Sigma-AldrichIRE1 Inhibitor IV, KIRA6 - CAS 1589527-65-0 - Calbiochem
KIRA6, IRE1a Kinase Inhibitor
More>> KIRA6, IRE1a Kinase Inhibitor Less<<MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: 1-(4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea, Kinase-Inhibiting RNase Attenuator 6, IRE1α Kinase Inhibitor
Recommended Products
Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 1589527-65-0 | C₂₈H₂₅F₃N₆O |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 5322810001 | Glass bottle | 10 mg |
| Description | |
|---|---|
| Overview | A cell-permeable, bioavailable, non-toxic, imidazopyrazinyl-naphthalenyl-phenylurea based compound that acts as a potent, ATP-competitive, reversible, and selective inhibitor of IRE1α kinase (IC50 = 600 nM). Exhibits good selectivity over ERK2, JNK2, JNK3, PIM1, PAK4, and PKA (IC50 > 10 µM). Stabilizes the kinase domain of IRE1α in an inactive conformation and blocks its oligomerization and thereby reduces RNase domain activity. Shown to block brefeldin A-(Cat. Nos. 203729 & 500583) induced ER stress and apoptosis in INS-1 cells and tunicamycin (Cat. Nos. 654380 & 504570)-induced apoptosis in β-cells derived from C57BL/6 mice. Affords significant cytoprotection in combination with STF-083010 (Cat. No. 412510, 1 µM) and KIRA6 (50 nM). Systemic administration of KIRA6 in the Akita diabetic mice is shown to reduce their blood glucose levels, improve glucose tolerance, and conserve their β-cell function. Preserves photoreceptor function in a transgenic rat model (P23H) of chronic ER stress-induced retinal degeneration, when administered intravitreally. Displays desirable pharmacokinetic properties with t1/2 = 3.9 h and moderate clearance rate of 22.4 ml/min/kg in BABL/c mice (10 mg/kg, i.p.). Please note that the molecular weight for this compound is batch-specific due to variable water content. |
| Catalogue Number | 532281 |
| Brand Family | Calbiochem® |
| Synonyms | 1-(4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea, Kinase-Inhibiting RNase Attenuator 6, IRE1α Kinase Inhibitor |
| References | |
|---|---|
| References | Ghosh, R., et al. 2014. Cell. 158, 534. |
| Product Information | |
|---|---|
| CAS number | 1589527-65-0 |
| Form | Off-white to brown powder |
| Hill Formula | C₂₈H₂₅F₃N₆O |
| Chemical formula | C₂₈H₂₅F₃N₆O |
| Reversible | Y |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Primary Target | IRE1α kinase |
| Purity | ≥95% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 5322810001 | 04055977260038 |