DRI-C21045 (compound 10) 是一种有效和选择性的 CD40-CD40L 共刺激蛋白-蛋白质相互作用 (PPI) 抑制剂，IC₅₀ 为 0.17 μM。DRI-C21045 显示对 CD40L 诱导的 NF-κB 活化和 B 细胞增殖的浓度依赖性抑制，IC₅₀ 分别为 17.1 μM 和 4.5 μM。

DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC 50 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 IC 50 s of 17.1 μM and 4.5 μM, respectively.

Solid

IC50: 0.17 μM (CD40)

DRI-C21045 (3.2-100 μM; 18 h) concentration-dependently inhibits the CD40L-induced NF-κB activation in CD40 sensor cells.
DRI-C21045 (0.6-50 μM; 48 h) blocks CD40L-induced functional activation of primary B cells.
DRI-C21045 (0.4-50 μM; 48 h) inhibits CD40L-induced MHC-II upregulation in THP-1 cells.
DRI-C21045 (2-100 μM; 48 h) inhibits CD40L-induced B cell proliferation.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

DRI-C21045 (30 mg/kg; daily, s.c.; in 20% HPβCD) prolongs graft survival in a murine allogeneic skin transplant model.
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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 2 mg/mL (3.44 mM; Need ultrasonic)配制储备液