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> Kira8 [1630086-20-2]

Kira8 [1630086-20-2]

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Cat# HY-114368-100mg

Size : 100mg

Brand : MedChemExpress

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

For research use only. We do not sell to patients.

Kira8 Chemical Structure

Kira8 Chemical Structure

CAS No. : 1630086-20-2

This product is a controlled substance and not for sale in your territory.

Based on 9 publication(s) in Google Scholar

Other Forms of Kira8:

  • Kira8 Hydrochloride Get quote
Description

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].

IC50 & Target

IRE1α[1]
IC50: 5.9 nM (IRE1α RNase)[1]
Cellular Effect
Cell Line Type Value Description References
HT-1080 IC50
0.099 μM
Compound: 18
Inhibition of human XBP1 splicing in human HT1080-CMV-XBP1-Luciferase cells assessed as luciferase signal by Promega Bright-Glo luciferase assay
Inhibition of human XBP1 splicing in human HT1080-CMV-XBP1-Luciferase cells assessed as luciferase signal by Promega Bright-Glo luciferase assay
[PMID: 25589933]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Kira8 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

601.12

Formula

C31H29ClN6O3S
CAS No.

1630086-20-2
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(OC4=NC=CC=C4C5=NC(N[C@@H]6CNCCC6)=NC=C5)C3=CC=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

Ethanol : 76.92 mg/mL (127.96 mM; ultrasonic and adjust pH to 5 with HCl)

DMSO : 65 mg/mL (108.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 30 mg/mL (49.91 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6636 mL 8.3178 mL 16.6356 mL
5 mM 0.3327 mL 1.6636 mL 3.3271 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 4 mg/mL (6.65 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  3% Ethanol    7% Tween-80    90% Saline

    Solubility: ≥ 2.31 mg/mL (3.84 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 5 mg/mL (8.32 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.60%

SDS (393 KB)

COA (256 KB) LCMS (91 KB)

Handling Instructions (2659 KB)
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.  [Content Brief]

  • [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.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO / Ethanol 1 mM 1.6636 mL 8.3178 mL 16.6356 mL 41.5890 mL
5 mM 0.3327 mL 1.6636 mL 3.3271 mL 8.3178 mL
10 mM 0.1664 mL 0.8318 mL 1.6636 mL 4.1589 mL
15 mM 0.1109 mL 0.5545 mL 1.1090 mL 2.7726 mL
20 mM 0.0832 mL 0.4159 mL 0.8318 mL 2.0795 mL
25 mM 0.0665 mL 0.3327 mL 0.6654 mL 1.6636 mL
30 mM 0.0555 mL 0.2773 mL 0.5545 mL 1.3863 mL
40 mM 0.0416 mL 0.2079 mL 0.4159 mL 1.0397 mL
DMSO / Ethanol 50 mM 0.0333 mL 0.1664 mL 0.3327 mL 0.8318 mL
60 mM 0.0277 mL 0.1386 mL 0.2773 mL 0.6932 mL
80 mM 0.0208 mL 0.1040 mL 0.2079 mL 0.5199 mL
100 mM 0.0166 mL 0.0832 mL 0.1664 mL 0.4159 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Kira8 Related Classifications

  • Cell Cycle/DNA Damage
  • IRE1
Help & FAQs

Keywords:

Kira81630086-20-2AMG-18Kira 8Kira-8AMG18AMG 18IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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