2. Cell Cycle/DNA Damage
  3. IRE1
  4. KIRA6

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

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

KIRA6 Chemical Structure

KIRA6 Chemical Structure

CAS No. : 1589527-65-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 137 In-stock
Solution
10 mM * 1 mL in DMSO USD 137 In-stock
Solid
1 mg USD 57 In-stock
5 mg USD 120 In-stock
10 mg USD 180 In-stock
50 mg USD 630 In-stock
100 mg USD 980 In-stock
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Customer Review

Based on 18 publication(s) in Google Scholar

KIRA6 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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 Kd 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.

KIRA6 Related Antibodies

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.
Molecular Weight

518.53

Formula

C28H25F3N6O
CAS No.
Appearance

Solid

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
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: 

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
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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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

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mg/kg

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(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.
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.
Purity & Documentation

Purity: 99.86%

SDS (393 KB)

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

Handling Instructions (2659 KB)
References

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
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
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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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