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CAS No. : 2101765-81-3
MCE 国际站:DRI-C21045
产品活性: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。
研究领域:Apoptosis
作用靶点:TNF Receptor
In Vitro: 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.
In Vivo: 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).
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货号: HY-120323
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