| Identification | Back Directory | [Name]
DRI-C21045
(DRI C21045) | [CAS]
2101765-81-3 | [Synonyms]
DRI-C21045
DRI-C21045
(DRI C21045)
8-(4'-(4-(Methoxycarbonyl)benzamido)-[1,1'-biphenyl]-4-carboxamido)naphthalene-1-sulfonic acid
8-(4'-(4-(Methoxycarbonyl)benzamido)-[1,1'-biphenyl]-4-carboxamido)naphthalene-1-sulfonic acid
DRI C21045,Tumor Necrosis Factor Receptor,DRI-C21045,DRIC21045,Inhibitor,DRI-C-21045,TNFR,inhibit,TNF Receptor
Benzoic acid, 4-[[[4'-[[(8-sulfo-1-naphthalenyl)amino]carbonyl][1,1'-biphenyl]-4-yl]amino]carbonyl]-, 1-methyl ester | [Molecular Formula]
C32H24N2O7S | [MDL Number]
MFCD32201050 | [MOL File]
2101765-81-3.mol | [Molecular Weight]
580.61 |
| Hazard Information | Back Directory | [Uses]
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 μM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 μM and 4.5 μM, respectively[1]. | [in vivo]
DRI-C21045 (30 mg/kg; daily, s.c.; in 20% HPβCD) prolongs graft survival in a murine allogeneic skin transplant model[1].
DRI-C21045 (20-60 mg/kg; twice daily s.c.; in 20% HPβCD) inhibits alloantigen-induced T cell expansion in the draining lymph nodes (DLNs)[1]. | Animal Model: | Full-thickness ear skins from BALB/c were transplanted onto the dorsal thorax of C57BL/6[1] | | Dosage: | 30 mg/kg | | Administration: | Daily s.c; administered in 20% w/v hydroxypropyl-β-cyclodextrin (HPβCD) solution | | Result: | Caused prolongation of skin allograft survival.
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| [References]
[1] Chen J, et al. Small-Molecule Inhibitors of the CD40-CD40L Costimulatory Protein-Protein Interaction. J Med Chem. 2017 Nov 9;60(21):8906-8922. DOI:10.1021/acs.jmedchem.7b01154
[2] Bojadzic D, et, al. Toward Small-Molecule Inhibition of Protein-Protein Interactions: General Aspects and Recent Progress in Targeting Costimulatory and Coinhibitory (Immune Checkpoint) Interactions. Curr Top Med Chem. 2018;18(8):674-699. DOI:10.2174/1568026618666180531092503 |
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