Kira8
CAS No. : 1630086-20-2
(Synonyms: AMG-18)
| Size | Price | Stock |
|---|---|---|
| 1mg | $110 | In-stock |
| 5mg | $260 | In-stock |
| 10mg | $390 | In-stock |
| 25mg | $720 | In-stock |
| 50mg | $1025 | In-stock |
| 100mg | $1405 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-114368 |
| M.Wt: | 601.12 |
| Formula: | C31H29ClN6O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 65 mg/mL (ultrasonic);Ethanol : 76.92 mg/mL (ultrasonic;adjust pH to 5 with HCl);H2O : 30 mg/mL (ultrasonic;warming;adjust pH to 2 with HCl;heat to 60°C) |
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].
IC50 & Target: IRE1α[1]
IC50: 5.9 nM (IRE1α RNase)[1]
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[1].
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[1].
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[1].
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