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Kira8 Hydrochloride

Catalog No. T11762 CAS 2250019-92-0

Synonyms: AMG-18 Hydrochloride

Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

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Kira8 Hydrochloride, CAS 2250019-92-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
Targets&IC50	IRE1α:, IRE1α RNase:5.9 nM
In vitro	Kira8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2.Kira8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs.
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. 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.

Synonyms	AMG-18 Hydrochloride
Molecular Weight	637.58
Formula	C31H30Cl2N6O3S
CAS No.	2250019-92-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Kira8 Hydrochloride 2250019-92-0 GPCR/G Protein Neuroscience Adenosine Receptor AMG-18 Hydrochloride Kira-8 Hydrochloride Inhibitor inhibitor inhibit

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