| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.17 µM (CD40) | ||||||||||||
| Invitro | DRI-C21045 (3.2-100 μM; 18 h) concentration-dependently inhibits the CD40L-induced NF-κB activation in CD40 sensor cells[1].DRI-C21045 (0.6-50 μM; 48 h) blocks CD40L-induced functional activation of primary B cells[1].DRI-C21045 (0.4-50 μM; 48 h) inhibits CD40L-induced MHC-II upregulation in THP-1 cells[1].DRI-C21045 (2-100 μM; 48 h) inhibits CD40L-induced B cell proliferation[1].DRI-C21045 shows no signs of cytotoxicity for concentrations of up to 100 and 200 µM and has no genotoxic potential for concentrations of up to 500 µM[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: | ||||||||||||
| Name | DRI-C21045 | ||||||||||||
| CAS | 2101765-81-3 | ||||||||||||
| Formula | C32H24N2O7S | ||||||||||||
| Molar Mass | 580.61 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. [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. |
DRI-C21045
CAS: 2101765-81-3 F: C32H24N2O7S W: 580.61
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction
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