KIRA6

Name: KIRA6
Brand: MedChemExpress
SKU: HY-19708
Rating: 5.0 (29 reviews)

Cat. No.: HY-19708 Purity: 98.75%: Data Sheet
COA

SDS
Handling Instructions
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KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC₅₀ of 0.6 µM. KIRA6 can trigger an apoptotic response.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1589527-65-0

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 29 publication(s) in Google Scholar

29 Publications Citing Use of MCE KIRA6

Cell Imaging/Staining

Cell Proliferation/Viability Assay

RT-PCR

: KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]; LX-2 cells were pre-treated with Kira6 (0.5 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h, V: Veh, K: Kira6, T: TGF-β1, K + T: Kira6 + TGF-β1. The levels of p-IRE1α and fibrosis-associated proteins were measured using western blotting.

: KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]; LX-2 cells were pre-treated with Kira6 (0.5 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h, V: Veh, K: Kira6, T: TGF-β1, K + T: Kira6 + TGF-β1. The mRNA levels of XBP1s.

: KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]; AML12 cells were pre-treated with Kira6 (1 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h. The levels of EMT-related proteins were detected using western blotting.

: KIRA6 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Nov 28;22(1):741. [Abstract]; AML12 cells were pre-treated with Kira6 (1 µM) for 1 h and stimulated with the corresponding inhibitor and TGF-β1 for 24 h. The mRNA levels of IL-6, IL-1β, TNF-α, and MCP-1 were measured by real-time PCR.

: KIRA6 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 May:272:120757.; KIRA6 (1.5 μM). TEM images of different liposomes. Scale bar, 100 nm.

: KIRA6 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2021 May:272:120757.; KIRA6 (0.5-15 μM). Cell viability of quiescent (naive) or activated (ɑ-CD3/28 Abs stimulation) splenic T-8 incubated with different liposomes at varying drug concentration for 24 h, respectively, n = 5.

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC₅₀ of 0.6 µM^[2]. KIRA6 can trigger an apoptotic response^[1].

IC₅₀ & Target

IC50: 0.6 µM (IRE1α RNase kinase)^[2]

In Vitro

KIRA6 (1nM-100μM) bounds to the cytoplasmic domain of KIT with a K_d value of 10.8 ?μM^[1].
? KIRA6 (10-1000 nM; 72 hours) strongly compromises the viability of the KIT-dependent cell line HMC-1.1 at the low nM concentration, in a manner that coincided with KIT blockade^[1].
? KIRA6 (10-1000 nM; 1 hour) reduces signaling output of KIT,? including the phosphorylation of KIT as well as its downstream signaling modules, PSTAT5 and phosphorylated ERK1/2^[1].
? KIRA6 (1 μM; 0-48 hours) inhibits Ins1 mRNA decay from IRE1α hyperactivation at a dose-dependent manner^[2].
? KIRA6 (0.1-10μM; 72 hours) dose-dependently reduces 1NM-PP1 potentiation of Ins1 apoptosis during ER stress in a dose-dependent manner^[2].

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

Cell Viability Assay^[1]

Cell Line:	HMC-1.1 cells
Concentration:	10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:	72 hours
Result:	Inhibited cell viability from 30 nM.

Western Blot Analysis^[1]

Cell Line:	HMC-1.1 cells
Concentration:	10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:	1 hours
Result:	Reduced expression of phosphorylated KIT, STAT5 and ERK1/2.

RT-PCR^[2]

Cell Line:	INS-1 IRE1α (WT) cells
Concentration:	1 μM
Incubation Time:	0 hour, 12 hours, 24 hours, 48 hours
Result:	Inhibited Ins1 mRNA expression.

Apoptosis Analysis^[2]

Cell Line:	INS-1 IRE1α (WT) cells
Concentration:	1-10 μM
Incubation Time:	72 hours
Result:	Reduced 1NM-PP1 potentiation of Ins1 apoptosis during ER stress.

In Vivo

KIRA6 (intraperitoneal injection; 5 mg/kg; 37 days) shows significant amelioration of random glucose levels over several weeks compared to vehicle, both fed ad lib^[2].
? KIRA6 (intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections) increases both plasma insulin and C-peptide levels, remains insulin-positive islet areas at high level after stopping injections in the Akita Mouse^[2].

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

Animal Model:	Male Ins2+/Akita mice^[2]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 21 or 18 days postinjections
Result:	Attenuates b cell functional loss, increased insulin levels.

분자량

518.53

화학식

C₂₈H₂₅F₃N₆O

CAS No.

1589527-65-0

Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=C3C=CC=CC3=C(C4=C5C(N)=NC=CN5C(C(C)(C)C)=N4)C=C2

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

용액&용해도

In Vitro:

DMSO : 25 mg/mL (48.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9285 mL	9.6426 mL	19.2853 mL
5 mM	0.3857 mL	1.9285 mL	3.8571 mL
10 mM	0.1929 mL	0.9643 mL	1.9285 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.

몰농도 계산기
농도 희석 계산기

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 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 (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.86%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (258 KB) HNMR (230 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Mahameed M,et al. The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis. 2019 Apr 1;10(4):300. [Content Brief]

[2]. Ghosh R, et al. Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress. Cell. 2014 Jul 31;158(3):534-48. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9285 mL	9.6426 mL	19.2853 mL	48.2132 mL
	5 mM	0.3857 mL	1.9285 mL	3.8571 mL	9.6426 mL
	10 mM	0.1929 mL	0.9643 mL	1.9285 mL	4.8213 mL
	15 mM	0.1286 mL	0.6428 mL	1.2857 mL	3.2142 mL
	20 mM	0.0964 mL	0.4821 mL	0.9643 mL	2.4107 mL
	25 mM	0.0771 mL	0.3857 mL	0.7714 mL	1.9285 mL
	30 mM	0.0643 mL	0.3214 mL	0.6428 mL	1.6071 mL
	40 mM	0.0482 mL	0.2411 mL	0.4821 mL	1.2053 mL

KIRA6 Related Classifications

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:

KIRA61589527-65-0KIRA 6KIRA-6IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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KIRA6

고객리뷰

KIRA6 Related Antibodies

29 Publications Citing Use of MCE KIRA6

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

순도&문서

References

고객리뷰

KIRA6 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

KIRA6 Related Classifications

Keywords:

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SAFETY DATA SHEET (SDS)

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