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Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $89 | In Stock | |
5 mg | $213 | In Stock | |
10 mg | $322 | In Stock | |
25 mg | $597 | In Stock | |
50 mg | $852 | In Stock | |
100 mg | $1,170 | In Stock | |
1 mL x 10 mM (in DMSO) | $283 | In Stock |
Description | Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. |
Targets&IC50 | IRE1α:5.9 nM(IRE1α RNase) |
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. |
Alias | AMG-18 |
Molecular Weight | 601.12 |
Formula | C31H29ClN6O3S |
Cas No. | 1630086-20-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 65 mg/mL (108.13 mM), Sonication is recommended. H2O: insoluble | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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