ZLDI-8 (ZLDI8, ZLDI 8)是一种Notch活化/裂解酶ADAM-17的抑制剂，抑制Notch蛋白的切割，降低了促生存/抗凋亡和EMT相关蛋白的表达。ZLDI-8还是一种不可逆的、竞争性的Lyp（酪氨酸磷酸酶）抑制剂，其IC₅₀值为31.6 μM，K_i值为26.22 μM。ZLDI-8能增强肝癌细胞对抑制剂索拉非尼、化疗药物依托泊苷和紫杉醇的敏感性。

参考文献

[1]. Li DD, Zhao CH, Ding HW, Wu Q, Ren TS, Wang J, Chen CQ, Zhao QC. A novel inhibitor of ADAM17 sensitizes colorectal cancer cells to 5-Fluorouracil by reversing Notch and epithelial-mesenchymal transition in vitro and in vivo. Cell Prolif. 2018 Oct;51(5): e12480. doi: 10.1111/cpr.12480. Epub 2018 Aug 2. PMID: 30069943; PMCID: PMC6528951.

[2]. Lu HY, Chu HX, Tan YX, Qin XC, Liu MY, Li JD, Ren TS, Zhang YS, Zhao QC. Novel ADAM-17 inhibitor ZLDI-8 inhibits the metastasis of hepatocellular carcinoma by reversing epithelial-mesenchymal transition in vitro and in vivo. Life Sci. 2020 Mar 1; 244:117343. doi: 10.1016/j.lfs.2020.117343. Epub 2020 Jan 21. PMID: 31978449.

[3]. Zhang Y, Li D, Jiang Q, Cao S, Sun H, Chai Y, Li X, Ren T, Yang R, Feng F, Li BA, Zhao Q. Novel ADAM-17 inhibitor ZLDI-8 enhances the in vitro and in vivo chemotherapeutic effects of Sorafenib on hepatocellular carcinoma cells. Cell Death Dis. 2018 Jul 3;9(7):743. doi: 10.1038/s41419-018-0804-6. PMID: 29970890; PMCID: PMC6030059.

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