| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| Z655325-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $385.90 |
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Biochemical and Physiological Mechanisms | ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a compet |
| Storage Temp | Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC 50 of 31.6 μM and a K i of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC 50 of 5.32 μM In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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 In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 days Result: Inhibited tumor growth in nude HCC-bearing mice model. IC50& Target:ADAM-17, IC50: 31.6 μM (Tyrosine phosphatase), Ki: 26.22 μM (Tyrosine phosphatase) |
| Canonical SMILES | CC1=CC(=C(C=C1)OCCN2C(=C(C3=CC=CC=C32)C=C4C(=O)NC(=S)NC4=O)C)C |
|---|---|
| Molecular Weight | 433.5 |
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