Formulation: A solid
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
Purity: ≥95%
Formula Markup: C34H33N7O10
Formula Weight: 699,7
Shelf life (days): 1460
CAS Number: 2762552-74-7
Notes: STING PROTAC SP23 is a proteolysis-targeting chimera (PROTAC) containing the stimulator of interferon genes (STING) inhibitor C-170 (Item No. 30157) conjugated to the cereblon (CRBN) inhibitor pomalidomide (Item No. 19877) via an α,β-unsaturated carbonyl linker.{72246} 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-β, 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 (Item No. 13119) when administered at doses of 30 and 60 mg/kg.
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