2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
IRE1α[1]
In Vivo
Kira8 efficaciously reverses established diabetes in NOD mice by sparing β-cells and preserving their physiological function. KIRA8 is first tested in 3-week-old male pre-diabetic Akita mice by i.p. daily dosing of 50 mg/kg, whereupon significant reduction of hyperglycemia became apparent over several weeks. Then KIRA8 (50 mg/kg) is tested in the complex NOD. Showing target engagement, one week treatment of pre-diabetic NODs with KIRA8 leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserved Ins1/Ins2, BiP and MANF mRNAs[1].
In Vitro
KIRA8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. KIRA8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2[1].
