| Description |
KIRA-7 is a small molecule inhibitor of IRE1α kinase/Rnase with IC50 of 0.11/0.22 uM, allosterically inhibits IRE1α RNase activity; reverses bleomycin-induced fibrosis when given 2 weeks after bleomycin exposure in vivo.
|
| Related Catalog |
|
| Target |
IC50: 110 nM (IRE1α kinase)[1]
|
| In Vitro |
KIRA-7 can inhibit XBP1 splicing in the alveolar epithelial cell line MLE12[1].
|
| 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[1]. Animal Model: C57BL6 mice (12 weeks of age) with Bleomycin (1.5 units/kg)[1] 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.
|
| References |
[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.
|
