GSK2850163

• CAT Number: I012902
• CAS Number: 2121989-91-9
• Molecular Formula: C₂₄H₂₉Cl₂N₃O
• Molecular Weight: 446.41
• Purity: ≥95%
• Target: IRE1
• Solubility: DMSO
• Storage: 2-8°C
• IUPAC Name: (5R)-2-[(3,4-dichlorophenyl)methyl]-N-[(4-methylphenyl)methyl]-2,7-diazaspiro[4.5]decane-7-carboxamide
• InChI: 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
• InChIKey: YFDASBFQKMHSSJ-XMMPIXPASA-N
• SMILES: CC1=CC=C(C=C1)CNC(=O)N2CCCC3(C2)CCN(C3)CC4=CC(=C(C=C4)Cl)Cl

GSK2850163（Cat No.:I012902） is a potent inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), an endoplasmic reticulum stress sensor involved in the unfolded protein response. It effectively inhibits both the kinase activity and RNase activity of IRE1α, with IC50 values of 20 and 200 nM, respectively. By blocking the activity of IRE1α, GSK2850163 modulates the unfolded protein response and may have therapeutic potential in diseases associated with aberrant protein folding and ER stress, such as cancer and neurodegenerative disorders.

Reference

[1]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.