Kira8

Research use only, not for human use.

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).(In Vitro):Kira8 more effectively causes IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2. Kira8 blocks IRE1α oligomerization and effectively inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs.(In Vivo):One week of treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) causes obvious reductions in islet XBP1 splicing and TXNIP mRNAs. It also preserves Ins1/Ins2, BiP, and MANF mRNAs. Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), obviously reduction of hyperglycemia becomes apparent over several weeks.

AMG-18

Others

Other Targets

antiprotozoal

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1630086-20-2

601.1

C31H29ClN6O3S

>98% (HPLC)

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Cc1ccc2c(NS(=O)(=O)c3ccccc3Cl)cccc2c1Oc1ncccc1-c1ccnc(N[C@H]2CCCNC2)n1

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(-20℃)

With Ice Pack

≥ 2 years