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Kira8

Catalog No. T11762L   CAS 1630086-20-2
Synonyms: AMG-18

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).

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Kira8 Chemical Structure
Kira8, CAS 1630086-20-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 89.00
5 mg In stock $ 213.00
10 mg In stock $ 322.00
25 mg In stock $ 597.00
50 mg In stock $ 852.00
100 mg In stock $ 1,170.00
1 mL * 10 mM (in DMSO) In stock $ 283.00
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Purity: 98.07%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
Targets&IC50 IRE1α:5.9 nM(IRE1α RNase)
In vitro Kira8 more effectively causes IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2. Kira8 blocks IRE1α oligomerization and effectively inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs.
In vivo One week of treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) causes obvious reductions in islet XBP1 splicing and TXNIP mRNAs. It also preserves Ins1/Ins2, BiP, and MANF mRNAs. Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), obviously reduction of hyperglycemia becomes apparent over several weeks.
Synonyms AMG-18
Molecular Weight 601.12
Formula C31H29ClN6O3S
CAS No. 1630086-20-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 65 mg/mL (108.13 mM), sonification is recommended.

H2O: insoluble

TargetMolReferences 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.

Related compound libraries

This product is contained In the following compound libraries:
Endoplasmic Reticulum Stress Compound Library Inhibitor Library Bioactive Compounds Library Max Kinase Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Cell Cycle Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets
MKC8866 GSK2850163 (S enantiomer) Sunitinib IRE1α kinase-IN-8 IRE1α kinase-IN-9 4μ8C Sunitinib Malate APY29

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Keywords

Kira8 1630086-20-2 Cell Cycle/Checkpoint IRE1 Inositol requiring enzyme 1 inhibit AMG-18 Kira 8 Inhibitor Kira-8 AMG 18 AMG18 inhibitor

 

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