2. Cell Cycle/DNA Damage
  3. IRE1
  4. IRE1α kinase-IN-1

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).

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

IRE1α kinase-IN-1 Chemical Structure

IRE1α kinase-IN-1 Chemical Structure

CAS No. : 2328097-41-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
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Based on 1 publication(s) in Google Scholar

IRE1α kinase-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM)[1].

In Vitro

IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells[1].
? IRE1α kinase-IN-1 and is very high selectivity with >70% inhibition of only 4/455 kinases. IRE1α kinase-IN-1 inhibits recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1].
? IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC50s ranging 0.68-1.63 μM[1].
? IRE1α kinase-IN-1 (0-20 μM) inhibits IRE1α-dependent XBP1s mRNA expression in H929 cells.IRE1α kinase-IN-1 (0-20 μM) dose-dependently inhibits tunicamycin-induced expression of XBP1s in NCI-H929 cells[1].

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

IRE1α kinase-IN-1 Related Antibodies
Molecular Weight

504.99

Formula

C26H26ClFN8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1CCC(CNC2=CC(Cl)=NN3C2=NC=C3C4=C(F)C=C5C(N=C(NC6=CC=CC=C6)N5)=C4)CC1
Shipping

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

DMSO : 25 mg/mL (49.51 mM; ultrasonic and warming and heat to 60°C; 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 1.9802 mL 9.9012 mL 19.8024 mL
5 mM 0.3960 mL 1.9802 mL 3.9605 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
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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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9802 mL 9.9012 mL 19.8024 mL 49.5059 mL
5 mM 0.3960 mL 1.9802 mL 3.9605 mL 9.9012 mL
10 mM 0.1980 mL 0.9901 mL 1.9802 mL 4.9506 mL
15 mM 0.1320 mL 0.6601 mL 1.3202 mL 3.3004 mL
20 mM 0.0990 mL 0.4951 mL 0.9901 mL 2.4753 mL
25 mM 0.0792 mL 0.3960 mL 0.7921 mL 1.9802 mL
30 mM 0.0660 mL 0.3300 mL 0.6601 mL 1.6502 mL
40 mM 0.0495 mL 0.2475 mL 0.4951 mL 1.2376 mL
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IRE1α kinase-IN-1 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:

IRE1α kinase-IN-12328097-41-0IRE1Inositol requiring enzyme 1autophosphorylationselectivityHEK293cellsoligomerizationendoribonucleaseendoplasmicreticulumInhibitorinhibitorinhibit

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