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

GSK2850163 

Cat. No.: HY-U00459 Purity: 98.50% ee.: 100.00%
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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 290 In-stock
Estimated Time of Arrival: December 31
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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].

Molecular Weight

446.41

Formula

C₂₄H₂₉Cl₂N₃O

CAS No.

2121989-91-9

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)

H2O : < 0.1 mg/mL (insoluble)

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 provided by MCE.
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

Purity: 98.50% ee.: 100.00%

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Product name:
GSK2850163
Cat. No.:
HY-U00459
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