K777  ≥98%

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包装规格:5mg in glass bottle
产品描述:一种有效的,口服活性且不可逆的半胱氨酸蛋白酶 (cysteine protease) 抑制剂,也是一种有效的 CYP3A4 抑制剂,IC50 为 60 nM,是一种选择性的 CCR4 拮抗剂,具有强的趋化性抑制作用。K-11777, also known as APC 3316; and K 777, is a a potent, irreversible cysteine protease inhibitor and a potent and selective CCR4 antagonist. Its therapeutic targets are cruzain, a cysteine protease of the protozoan parasite Trypanosoma cruzi, and cathepsins B and L, which are associated with cancer progression. K777 inhibited both CCL17 binding and CCL17-induced chemotaxis in Hut78 cells (IC50: 57 and 8.9 nmol/l, respectively). K777 induced CCR4 internalization, with a ∼50% reduction of cell surface CCR4. K777 did not inhibit CXCR4-induced chemotaxis or internalization and did not bring about Ca(2+) mobilization by itself.
保存条件:-20℃