ZLDI-8

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ZLDI-8 是 Notch 激活/裂解酶 ADAM-17 的抑制剂，可抑制 Notch 蛋白的裂解。ZLDI-8；它抑制NOTCH蛋白的裂解，从而降低促生存/抗凋亡和EMT相关蛋白的表达。

ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.ZLDI-8;?it inhibited the cleavage of NOTCH protein, consequently decreased the expression of pro-survival/anti-apoptosis and EMT related proteins.?ZLDI-8 treatment enhanced the susceptibility of HCC cells to a small molecular kinase inhibitor Sorafenib, and chemotherapy agents Etoposide and Paclitaxel.?ZLDI-8 treatment enhanced the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model.?In nude HCC-bearing mice model, ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth.

ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner.ZLDI-8 (1-10 μM; 6-72 hours; MHCC97-H cells) significantly decreases the level of NICD and the accumulation of NICD in the nucleus. ZLDI-8 could also reduce the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2. And also increases the expression of epithelial marker E-Cadherin and reduced mesenchymal markers N-Cadherin and Vimentin.ZLDI-8 enhances chemotherapy effects on tumor cell proliferation blockage, induction of apoptosis and cell-cycle arrest by inhibiting Notch pathway and blocking chemical resistance. Cell Viability Assay Cell Line:MHCC97-H cells Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM Incubation Time:6 hours, 12 hours, 24 hours, 48 hours, 72 hours Result:Emerged cytotoxic effect on MHCC97-H cells in a time- and dose-dependent manner.Western Blot Analysis Cell Line:MHCC97-H cells Concentration:1 μM, 3 μM, 10 μM Incubation Time:6 hours, 12 hours, 24 hours, 48 hours, 72 hours Result:Significantly decreased the level of NICD and the accumulation of NICD in the nucleus. Also reduced the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2

ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model. Animal Model:Nude mice with MHCC-97H cells Dosage:2?mg/kg, 1?mg/kg, 500?μg/kg, or 200?μg/kg Administration:Intraperitoneal injection; every two days; for 20 daysResult: Inhibited tumor growth in nude HCC-bearing mice model.

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Others

Other Targets

ADAM-17

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667880-38-8

433.52

C24H23N3O3S

>98% (HPLC)

DMSO:62.5 mg/mL (144.17 mM; Need ultrasonic)

O=C(/C(C(N1)=O)=C/C2=C(C)N(CCOC3=CC=C(C)C=C3C)C4=C2C=CC=C4)NC1=S

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(-20℃)

With Ice Pack

≥ 2 years