名称 | DZ2002 |
描述 | DZ2002, an orally active, reversible, and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), exhibits significant immunosuppressive activity. It effectively prevents experimental dermal fibrosis by reversing the profibrotic phenotype in multiple cell types, making it useful for studying autoimmune diseases like lupus syndrome and systemic sclerosis. |
体外活性 | DZ2002 (0.1, 1, 10 µM; 96 h) inhibits the mixed lymphocyte reaction (MLR) response, IL-12 and TNF-α production from both mouse peritoneal exudate cells and human THP-1 cells (24 h), and expression of B7 (CD80/CD86) on differentiated THP-1 cells (64 h) [1]. |
体内活性 | DZ2002 (2, 10, 50 mg/kg; i.p.; twice) blocks the DNFB-induced DTH response—a Th1 cell-mediated immune response with high IL-12 expression and significant macrophage involvement. DZ2002 (0.08, 2 mg/kg; i.p.; daily for 7 days) significantly suppresses delayed-type hypersensitivity and antibody secretion[1]. DZ2002 (50, 100 mg/kg; p.o.; daily for 4 weeks) exhibits a potent anti-fibrotic effect on dermal fibrosis by reducing collagen production, enhancing its degradation, and regulating various soluble factors in SSc mice model[2]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 45 mg/mL (179.11 mM), Sonication is recommended.
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关键字 | DZ-2002 | DZ2002 | DZ 2002 |
相关库 | 经典已知活性库 | 抑制剂库 | 抗纤维化化合物库 | 口服活性化合物库 | 免疫/炎症分子化合物库 | 已知活性化合物库 |