KIRA-7 (C09-1141-473)

KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase ( IC 50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effectIn VitroKIRA-7 can inhibit XBP1 splicing in the alveolar epithelial cell line MLE12. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoKIRA-7 (5 mg/kg; intraperitoneal injection; daily for 14 days; C57BL6 mice) treatment results in decreased spliced XBP1 and ATF4, compared to bleomycin exposed mice treated with vehicle. Likewise, mRNA levels of BiP and CHOP are significantly elevated after Bleomycin exposure, and treatment of Bleomycin-exposed mice with KIRA-7 decreased these levels. mRNA levels of collagen 1A1 and fibronectin are both significantly decreased by KIRA-7 treatment . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL6 mice (12 weeks of age) with Bleomycin (1.5 units/kg) Dosage: 5 mg/kg Administration: Intraperitoneal injection; daily; for 14 days Result: Resulted in decreased spliced XBP1 and ATF4. Likewise, mRNA levels of BiP and CHOP were significantly decreased.Form:SolidIC50& Target:IC50: 110 nM (IRE1α kinase). Specification: 0.98 Molecular Formula: C27H23FN6O Molecular Weight: 466.51