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Kira8

Catalog No. T11762LCas No. 1630086-20-2
Alias AMG-18

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

Kira8

Kira8

Purity: 98.07%
Catalog No. T11762LAlias AMG-18Cas No. 1630086-20-2
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
Pack SizePriceAvailabilityQuantity
1 mg$89In Stock
5 mg$213In Stock
10 mg$322In Stock
25 mg$597In Stock
50 mg$852In Stock
100 mg$1,170In Stock
1 mL x 10 mM (in DMSO)$283In Stock
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Purity:98.07%
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Product Introduction

Bioactivity
Description
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 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.
AliasAMG-18
Chemical Properties
Molecular Weight601.12
FormulaC31H29ClN6O3S
Cas No.1630086-20-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 65 mg/mL (108.13 mM), Sonication is recommended.
H2O: insoluble
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6636 mL8.3178 mL16.6356 mL83.1781 mL
5 mM0.3327 mL1.6636 mL3.3271 mL16.6356 mL
10 mM0.1664 mL0.8318 mL1.6636 mL8.3178 mL
20 mM0.0832 mL0.4159 mL0.8318 mL4.1589 mL
50 mM0.0333 mL0.1664 mL0.3327 mL1.6636 mL
100 mM0.0166 mL0.0832 mL0.1664 mL0.8318 mL

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