Kira8 Hydrochloride
Modify Date: 2024-01-11 09:16:26
Kira8 Hydrochloride structure
|
Common Name | Kira8 Hydrochloride | ||
|---|---|---|---|---|
| CAS Number | 2250019-92-0 | Molecular Weight | 637.58 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C31H30Cl2N6O3S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Kira8 HydrochlorideKira8 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 |