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 effect.
性状
Solid
IC50 & Target[1][2]
IC50: 110 nM (IRE1α kinase)
体外研究(In Vitro)
KIRA-7 can inhibit XBP1 splicing in the alveolar epithelial cell line MLE12. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
KIRA-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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Thamsen M, et al. Small molecule inhibition of IRE1α kinase/RNase has anti-fibrotic effects in the lung. PLoS One. 2019 Jan 9;14(1):e0209824.