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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $793 | 35 days |
Description | Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. |
Targets&IC50 | IRE1α:, IRE1α RNase:5.9 nM |
In vitro | Kira8 more effectively diminishes IRE1α-driven apoptosis in INS-1 cells compared to KIRA6 and additionally counteracts XBP1 splicing induced by GNF-2. It inhibits IRE1α oligomerization and significantly reduces IRE1α RNase activity targeting XBP1 and Ins2 RNAs. |
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. |
Alias | AMG-18 Hydrochloride |
Molecular Weight | 637.58 |
Formula | C31H30Cl2N6O3S |
Cas No. | 2250019-92-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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