Kira8

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC 50 of 5.9 nM 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Male Ins2 +/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks . One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Ins2 +/Akita mice Dosage: 50 mg/kg Administration: Injected i.p.; daily; for 35 days Result: Significant reduction of hyperglycemia became apparent over several weeks. IC50& Target:IRE1α, IC50: 5.9 nM (IRE1α RNase)

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