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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. |
| Synonyms | AMG-18 |
| Molecular Weight | 601.12 |
| Formula | C31H29ClN6O3S |
| Cas No. | 1630086-20-2 |
| Smiles | Cc1ccc2c(NS(=O)(=O)c3ccccc3Cl)cccc2c1Oc1ncccc1-c1ccnc(N[C@H]2CCCNC2)n1 |
| Relative Density. | 1.383 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 65 mg/mL (108.13 mM), Sonication is recommended. H2O: insoluble | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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