Isogarcinol is a natural polyisoprenylated benzophenone first isolated from plant species in the genus Garcinia. It has immunosuppressant actions, inhibiting the protein phosphatase calcineurin (IC50 = 36 μM) and suppressing the proliferation of T cells. Oral administration of isogarcinol in mice decreases delayed type hypersensitivity, prolongs graft survival in allogeneic skin transplants, suppresses inflammation in collagen-induced arthritis, and reduces clinical symptoms in experimental autoimmune encephalomyelitis. Isogarcinol inhibits the proliferation of HL-60 and PC-3 cancer cells (IC50s = 4 and 8 μg/ml, respectively) through cell cycle arrest and apoptosis.
Dibefurin is a metabolite that inhibits the activity of calcineurin, a calcium/calmodulin-dependent protein phosphatase involved in the activation of T lymphocytes.
Cyclosporin Aacetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) 是一种氘代Cyclosporin A。Cyclosporin A (Cyclosporine A) 是免疫抑制剂,通过与亲环素结合,抑制protein phosphatase 2B (PP2B/calcineurin) 的活性,IC50为7 nM。其还对粘附分子CD11a/CD18有抑制作用。
Cyclosporin D is a metabolite of cyclosporin A, an immunosuppressant drug that binds cyclophilin D, inhibiting the phosphatase activity of calcineurin in T cells.
Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 μM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).