Kira8 Hydrochloride

Modify Date: 2024-01-11 09:16:26

Kira8 Hydrochloride Structure
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 Hydrochloride


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].

 Names

Name Kira8 Hydrochloride

 Kira8 Hydrochloride Biological Activity

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

[1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8.

 Chemical & Physical Properties

Molecular Formula C31H30Cl2N6O3S
Molecular Weight 637.58