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

GSK2850163 

Cat. No.: HY-U00459 Purity: 98.48%
COA Handling Instructions

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

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Oil + Solvent
10 mM * 1 mL
ready for reconstitution
 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
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500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of GSK2850163:

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

446.41

Appearance

Oil

Formula

C24H29Cl2N3O
CAS No.
SMILES

O=C(N(CCC1)C[[email protected]]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)

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
10 mM 0.2240 mL 1.1200 mL 2.2401 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.48%

COA (246 KB) RP-HPLC (257 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
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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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

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