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.

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].

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].