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KIRA6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 µM. KIRA6 inhibits IRE1α auto-phosphorylation by Tg and XBP1 mRNA splicing by Tm in a dose-dependent manner in INS-1 cells. KIRA6 (10-1000 nM; 72 hours) strongly compromises the viability of the KIT-dependent cell line HMC-1.1 at the low nM concentration, in a manner that coincided with KIT blockade. KIRA6 (10-1000 nM; 1 hour) reduces signaling output of KIT, including the phosphorylation of KIT as well as its downstream signaling modules, PSTAT5 and phosphorylated ERK1/2. In vivo, KIRA6 inhibits IRE1α to preserve cell viability and function in diverse cells and rodent tissues experiencing ER stress. KIRA6 (intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at high level after stopping injections in the Akita Mouse.
| Molecular Weight | 518.53 |
| Formula | C28H25F3N6O |
| CAS Number | 1589527-65-0 |
| Solubility (25°C) | DMSO ≥ 6 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IRE1 Products |
|---|
| BDM44768
BDM44768 is an inhibitior of IDE. |
| IRE1α kinase-IN-5
IRE1α kinase-IN-5 is a potent IRE1α inhibitor with an Ki of 98 nM. |
| Z4P
Z4P is a BBB-permeable IRE1 inhibitor (IC50: 1.11 μM). |
| IRE1α kinase-IN-9
IRE1α kinase-IN-9 is a potent IRE-1α inhibitor, exhibits an average IC50 value of <0.1 μM. |
| IRE1α kinase-IN-8
IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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