KGP94是一种特异性 cathepsin L 抑制剂，IC50 值为 189 nM，能抑制癌细胞的迁移和侵袭，同时对正常人类细胞的毒性较低 (GI50=26.9µM)，适用于癌症转移研究。
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KGP94 is a selective cathepsin L inhibitor with an IC50 value of 189 nM[1].KGP94 inhibits migration and invasion of metastatic cancers and shows low cytotoxicity against a variety of human cell lines (GI50=26.9 µM)[2].At concentrations of 10 µM or 20 µM, acting for 24 hours, KGP94 reduces the expression of markers of macrophage M2 (arginase-1 and CD206) as well as cellular invasion by primary bone marrow-derived macrophages or Raw264.7[3].At a concentration of 25 μM for 24 hours of treatment, the effects of KGP94 on the invasive capacity of prostate and respiratory cancer cells were 53% and 88%, respectively, and the inhibition of CTSL activity secreted by PC-3ML and MDA-MB-231 was 94% and 92%, respectively[4].
KGP94 动物研究
Animal study
At a dose of 20 mg/kg, injected intraperitoneally once a day for 3 days, KGP94 showed anti-metastatic and anti-bone resorption efficacy in a bone metastasis model of prostate cancer. Metastatic tumour burden was reduced by 65%, tumour angiogenesis was reduced by 58%, and survival was improved in mice with bone metastases[5].
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