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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 |
|---|
| 4μ8C
4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM. |
| STF-083010
STF-083010 is a potent inhibitor of the ER transmembrane protein IRE1, which mediates the unfolded protein response. |
| MKC-3946
MKC-3946 is a potent IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines. |
| Kira8
Kira8 (AMG-18) is a single selective IRE1α inhibitor with an IC50 of 5.9 nM. |
| GSK2850163
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. |
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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