1. Cell Cycle/DNA Damage
  2. IRE1

GSK2850163 hydrochloride 

Cat. No.: HY-U00459B
Handling Instructions

GSK2850163 hydrochloride 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 hydrochloride Chemical Structure

GSK2850163 hydrochloride Chemical Structure

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5 mg USD 160 Get quote
10 mg USD 280 Get quote
25 mg USD 560 Get quote

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Other Forms of GSK2850163 hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK2850163 hydrochloride 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 hydrochloride 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 can be reduced in a dose-dependent manner by GSK2850163 hydrochloride. Increasing concentrations of GSK2850163 hydrochloride are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163 hydrochloride: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM)[1].

References
Kinase Assay
[1]

In the ADP-Glo assay, GSK2850163 hydrochloride’s potency toward pIRE1α kinase activity is measured as its inhibition of an intrinsic, slowing ATP hydrolysis activity. One hundred nanoliters of dimethylsulfoxide solution of GSK2850163 hydrochloride at various concentrations is added into a 384-well plate. The reaction is carried out with 5 nM pIRE1α and 60 mM ATP in 10 mL of 50 mM Hepes buffer, pH 7.5, containing 30 mM NaCl, 10 mM MgCl2, 1 mM DTT, 0.02% Chaps, and 0.01 mg/mL bovine serum albumin. The reaction is stopped after 2 hours by adding 5 mL of ADP-Glo reagent I, which also depletes the remaining ATP. Following 1-hour incubation, 5 mL of ADP-Glo reagent II is added into the reaction, which converts the ADP product into ATP to serve as the substrate for the coupled luciferin/luciferase reaction. After 30 minutes, the plate is read on a microplate imager[1].

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

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 hydrochloride 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
Molecular Weight

482.87

Formula

C₂₄H₃₀Cl₃N₃O

SMILES

O=C(N(CCC1)C[[email protected]]21CCN(CC3=CC=C(Cl)C(Cl)=C3)C2)NCC4=CC=C(C)C=C4.Cl

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GSK2850163 hydrochloride
Cat. No.:
HY-U00459B
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GSK2850163 hydrochloride

Cat. No.: HY-U00459B