2250019-92-0
2250019-92-0 structure
- Name: Kira8 Hydrochloride
- Chemical Name: Kira8 Hydrochloride
- CAS Number: 2250019-92-0
- Molecular Formula: C31H30Cl2N6O3S
- Molecular Weight: 637.58
- Catalog: Signaling Pathways Cell Cycle/DNA Damage IRE1
- Create Date: 2019-12-08 19:31:32
- Modify Date: 2024-01-11 09:16:26
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Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].
| Name | Kira8 Hydrochloride |
|---|
| Description | Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1]. |
|---|---|
| Related Catalog | |
| 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]. Animal Model: Male Ins2+/Akita mice[1] Dosage: 50 mg/kg Administration: Injected i.p.; daily; for 35 days Result: Significant reduction of hyperglycemia became apparent over several weeks. |
| References |
| Molecular Formula | C31H30Cl2N6O3S |
|---|---|
| Molecular Weight | 637.58 |