DZ2002 是一种口服有效的、可逆的、低细胞毒性的 III 型 SAHH 抑制剂 (Ki=17.9 nM)，具有较好的免疫抑制活性。DZ2002 能通过逆转各种细胞类型的促纤维化表型来防止实验性皮肤纤维化的发展。DZ2002 可用于自身免疫性疾病，如狼疮综合征和系统性硬化症的研究。

DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.

DZ2002 (0.1, 1, 10 μM; 96 h) inhibits the mixed lymphocyte reaction (MLR) response. DZ2002 (0.1, 1, 10 μM; 24 h) inhibits IL-12 and TNF-α production from both mouse peritoneal exudate cells and humanTHP-1 Cells. DZ2002 (0.1, 1, 10 μM; 64 h) inhibits expression of B7 (CD80/CD86) on differentiated THP-1 cells[1].

DZ2002 (2, 10, 50 mg/kg; i.p.; twice) blocks the DNFB-induced DTH response. (DNFB-induced DTH is a Th1 cell-mediated immune response, in which IL-12 is highly expressed and macrophages have been shown to play an important role). DZ2002 (0.08, 2 mg/kg; i.p.; single daily for 7 days) significantly suppresses a delayed-type hypersensitivity reaction as well as antibody secretion[1]. DZ2002 (50, 100 mg/kg; p.o.; single daily for 4 weeks) exerts a potent anti-fibrotic effect on dermal fibrosis by reducing the production of collagen, facilitating its degradation and regulating expression of various soluble factors in SSc mice model[2].

33231-14-0

C10H13N5O3

251.24

DZ2002

DMSO:54.9mg/mL (218.5mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years