An IRE1α inhibitor
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GSK2850163

Item No. 40917

Technical Information
Formal Name
2-[(3,4-dichlorophenyl)methyl]-N-[(4-methylphenyl)methyl]-2,7-diazaspiro[4.5R]decane-7-carboxamide
CAS Number
2121989-91-9
Synonyms
  • GSK163
Molecular Formula
C24H29Cl2N3O
Formula Weight
Purity
≥98%
A solution in ethanol
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(N1CCC[C@@]2(CN(CC3=CC(Cl)=C(Cl)C=C3)CC2)C1)NCC4=CC=C(C)C=C4
InChi Code
InChI=1S/C24H29Cl2N3O/c1-18-3-5-19(6-4-18)14-27-23(30)29-11-2-9-24(17-29)10-12-28(16-24)15-20-7-8-21(25)22(26)13-20/h3-8,13H,2,9-12,14-17H2,1H3,(H,27,30)/t24-/m1/s1
InChi Key
YFDASBFQKMHSSJ-XMMPIXPASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    GSK2850163 is an inhibitor of inositol-requiring enzyme 1α (IRE1α; IC50s = 0.2 and 0.02 µM for RNase and kinase activity, respectively).1 It is selective for IRE1α over Ron and FGFR1 (IC50s = 4.4 and 17 µM), as well as a panel of 282 kinases at 10 µM. GSK2850163 (8 µM) inhibits endoplasmic reticulum (ER) stress-induced increases in the splicing of mRNA encoding X-box binding protein 1 (XBP1) in eight multiple myeloma cell lines. It reduces viral replication in tick-borne encephalitis virus-infected SH-SY5Y and SNB-19 cells when used at a concentration of 0.5 µM or tick-borne encephalitis virus-infected Caco-2 cells at 1 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Concha, N.O., Smallwood, A., Bonnette, W., et alLong-range inhibitor-induced conformational regulation of human IRE1α endoribonuclease activity. Mol. Pharmacol. 88(6), 1011-1023 (2015).

    2. Breitkopf, V.J.M., Dobler, G., Claus, P., et alIRE1-Mediated unfolded protein response promotes the replication of tick-borne flaviviruses in a virus and cell-type dependent manner. Viruses 13(11), 2164 (2021).