STING PROTAC SP23

STING PROTAC SP23 is a proteolysis-targeting chimera (PROTAC) containing the stimulator of interferon genes (STING) inhibitor C-170 (Cay-30157) conjugated to the cereblon (CRBN) inhibitor pomalidomide (Cay-19877) via an alpha,beta-unsaturated carbonyl linker. It degrades STING in THP-1 cells with a half-maximal degradation concentration (DC50) of 3.2 µM, an effect that can be blocked by the proteasome inhibitor MG132 but not the lysosome inhibitor bafilomycin. STING PROTAC SP23 (2.5-20 µM) decreases cGAMP-induced increases in the levels of IFN-beta, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells. It also reduces kidney weight, improves kidney function, and increases the survival rate in a mouse model of acute kidney injury induced by the DNA-crosslinking agent cisplatin (Cay-13119) when administered at doses of 30 and 60 mg/kg.Formal Name: (2E)-N1-[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]hexyl]-N4-[4-[[(5-nitro-2-furanyl)carbonyl]amino]phenyl]-2-butenediamide. CAS Number: 2762552-74-7. Synonyms: PROTAC Stimulator of Interferon Genes Degrader-1, PROTAC STING Degrader-1, Proteolysis-targeting Chimera Stimulator of Interferon Genes Degrader-1, Proteolysis-targeting Chimera STING Degrader-1, Stimulator of Interferon Genes PROTAC SP23, Stimulator of Interferon Genes Proteolysis-targeting Chimera SP23, STING Proteolysis-targeting Chimera SP23. Molecular Formula: C34H33N7O10. Formula Weight: 699.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble. SMILES: O=C(N1C(CCC2=O)C(N2)=O)C(C(C1=O)=CC=C3)=C3NCCCCCCNC(/C=C/C(NC(C=C4)=CC=C4NC(C5=CC=C([N+]([O-])=O)O5)=O)=O)=O. InChi Code: InChI=1S/C34H33N7O10/c42-26(15-16-27(43)37-20-8-10-21(11-9-20)38-32(46)25-13-17-29(51-25)41(49)50)36-19-4-2-1-3-18-35-23-7-5-6-22-30(23)34(48)40(33(22)47)24-12-14-28(44)39-31(24)45/h5-11,13,15-17,24,35H,1-4,12,14,18-19H2,(H,36,42)(H,37,43)(H,38,46)(H,39,44,45)/b16-15+. InChi Key: TXNQXRGOKABDOB-FOCLMDBBSA-N.