2. Cell Cycle/DNA Damage
  3. IRE1
  4. GSK2850163

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

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

GSK2850163 Chemical Structure

GSK2850163 Chemical Structure

CAS No. : 2121989-91-9

Size Price Stock Quantity
Oil + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Oil
5 mg USD 80 In-stock
10 mg USD 140 In-stock
25 mg USD 290 In-stock
50 mg USD 460 In-stock
100 mg USD 740 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of GSK2850163:

GSK2850163 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

IC50 & Target

IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)[1]
In Vitro

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. The increased autophosphorylation of IRE1α could be reduced in a dose-dependent manner by GSK2850163. Increasing concentrations of GSK2850163 are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM)[1].

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

GSK2850163 Related Antibodies
Molecular Weight

446.41

Formula

C24H29Cl2N3O
CAS No.
Appearance

Oil

Color

Colorless to yellow

SMILES

O=C(N(CCC1)C[C@]21CCN(CC3=CC=C(Cl)C(Cl)=C3)C2)NCC4=CC=C(C)C=C4
Shipping

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

DMSO : 67.5 mg/mL (151.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (112.00 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2401 mL 11.2005 mL 22.4009 mL
5 mM 0.4480 mL 2.2401 mL 4.4802 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)

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.25 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: ≥ 2.25 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 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 (22.5 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)

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: 98.43%

COA (246 KB) RP-HPLC (246 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

PANC-1 cells are seeded into six-well plates at a density of 5.0×103 cells/well in RPMI 1640 media containing 10% FBS. Cells are cotransfected with a pGL3-5x unfolded protein response element (UPRE)-luciferase reporter containing five repetitions of the XBP-1 DNA binding site and pRL-SV40 using the FuGENE6 transfection reagent. Forty-eight hours later, cells are treated with 2.5 mg/mL tunicamycin for 1 hour, followed by GSK2850163 treatment for 16 hours. Luciferase expression is measured using Dual-Glo Luciferase Assay kit and normalized to Renilla expression levels[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
Ethanol / DMSO 1 mM 2.2401 mL 11.2005 mL 22.4009 mL 56.0023 mL
5 mM 0.4480 mL 2.2401 mL 4.4802 mL 11.2005 mL
10 mM 0.2240 mL 1.1200 mL 2.2401 mL 5.6002 mL
15 mM 0.1493 mL 0.7467 mL 1.4934 mL 3.7335 mL
20 mM 0.1120 mL 0.5600 mL 1.1200 mL 2.8001 mL
25 mM 0.0896 mL 0.4480 mL 0.8960 mL 2.2401 mL
30 mM 0.0747 mL 0.3733 mL 0.7467 mL 1.8667 mL
40 mM 0.0560 mL 0.2800 mL 0.5600 mL 1.4001 mL
50 mM 0.0448 mL 0.2240 mL 0.4480 mL 1.1200 mL
60 mM 0.0373 mL 0.1867 mL 0.3733 mL 0.9334 mL
80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.7000 mL
100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5600 mL
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GSK2850163 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:

GSK28501632121989-91-9GSK 2850163GSK-2850163IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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