Kira8 (Synonyms: AMG-18)

Name: Kira8
Brand: MedChemExpress
SKU: HY-114368
Rating: 5.0 (14 reviews)

Cat. No.: HY-114368 Purity: 98.90%: Data Sheet
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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.

CAS No. : 1630086-20-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Kira8:

Kira8 Hydrochloride In-stock

14 Publications Citing Use of MCE Kira8

Cell Imaging/Staining

Bio/Physico-chemical Assay

: Kira8 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 May 8;51(8):3650-3670. [Abstract]; FXBP1s expression. Western immunoblot of hSAECs transduced with empty (pCT) or FXBP1s-expressing lentiviral vector at an MOI of 2.0 for 48 h, or mock-treated or treated with tunicamycin (TM, 0.5 μg/ml for 8 h) or thapsigargin (Tg, 50 nM for 6 h) in the absence or presence of KIRA8 (10 μM). Nuclear extracts were prepared and stained with anti-FLAG M2 or anti-XBP1s antibodies. TBP was used as loading control.

: Kira8 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 May 8;51(8):3650-3670. [Abstract]; We observed that Tg induced a 3.5 ± 0.5-fold increase in endogenous XBP1s binding to the GFPT1 promoter. This induction was completely inhibited by the treatment with KIRA8 (10 μM).

: Kira8 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]; In a manner similar to our observations on the RSV induction of cell-associated FN1, we found that FN1 deposition into the ECM was also blocked by KIRA8 (10 μM, pre-treated for two hours).

: Kira8 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]; Principal component analysis of significant proteins (ANOVA with permutation-based FDR < 0.01). Green circle, controls; red square, RSV infection; blue diamond, RSV infection + KIRA8 treatment.

: Kira8 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000. [Abstract]; Proteomics analysis of N-glycosylation in hSAECs infected with RSV in the presence or absence of KIRA8. hSAECs were infected with RSV at 1.0 MOI for 24 h in the presence or absence of KIRA8 (10 µM). The N-glycosylated peptides were enriched with lectins and then analyzed with label-free LC-MS/MS. Volcano plot of N-glycosylated peptides (RSV vs. Control). Red circle, N-glycoproteins upregulated by RSV; green square, N-glycoproteins downregulated by RSV infection.

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Biological Activity
Purity & Documentation
References
Customer Review

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.

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

Off-white 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
10 mM	0.1664 mL	0.8318 mL	1.6636 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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: 98.90%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (256 KB) HNMR (181 KB) RP-HPLC (140 KB) LCMS (235 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]

Complete Stock Solution Preparation Table

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.

Kira8 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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Kira8 (Synonyms: AMG-18)

Customer Review

Other Forms of Kira8:

Kira8 Related Antibodies

14 Publications Citing Use of MCE Kira8

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Kira8 Related Antibodies

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Complete Stock Solution Preparation Table

Kira8 Related Classifications

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