ZLDI-8
Based on 1 publication(s) in Google Scholar
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 IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
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- Pureza: 98.47%
- No. CAS: 667880-38-8
- Fòrmula: C24H23N3O3S
- Peso molecular:433.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) ZLDI-8
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Actividad biológica
ADAM-17[1]
IC50: 31.6 μM (Tyrosine phosphatase)[1]
Ki: 26.22 μM (Tyrosine phosphatase)[1]
ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner[1].
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[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MHCC97-H cells
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Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
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Incubation Time:6 hours, 12 hours, 24 hours, 48 hours, 72 hours
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Result:Emerged cytotoxic effect on MHCC97-H cells in a time- and dose-dependent manner.
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Cell Line:MHCC97-H cells
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Concentration:1 μM, 3 μM, 10 μM
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Incubation Time:6 hours, 12 hours, 24 hours, 48 hours, 72 hours
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice with MHCC-97H cells[1]
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Dosage:2 mg/kg, 1 mg/kg, 500 μg/kg, or 200 μg/kg
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Administration:Intraperitoneal injection; every two days; for 20 days
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Result:Inhibited tumor growth in nude HCC-bearing mice model.
Chemical Information
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No. CAS 667880-38-8
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Appearance Solid
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Peso molecular 433.52
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Fòrmula C24H23N3O3S
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Color Yellow to orange
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SMILES
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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 62.5 mg/mL (144.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhang Y, et al. 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. [Content Brief]
[2]. Hou X, et al. Fast identification of novel lymphoid tyrosine phosphatase inhibitors using target-ligand interaction-based virtual screening. J Med Chem. 2014 Nov 26;57(22):9309-22. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3067 mL | 11.5335 mL | 23.0670 mL | 57.6675 mL |
| 5 mM | 0.4613 mL | 2.3067 mL | 4.6134 mL | 11.5335 mL | |
| 10 mM | 0.2307 mL | 1.1533 mL | 2.3067 mL | 5.7667 mL | |
| 15 mM | 0.1538 mL | 0.7689 mL | 1.5378 mL | 3.8445 mL | |
| 20 mM | 0.1153 mL | 0.5767 mL | 1.1533 mL | 2.8834 mL | |
| 25 mM | 0.0923 mL | 0.4613 mL | 0.9227 mL | 2.3067 mL | |
| 30 mM | 0.0769 mL | 0.3844 mL | 0.7689 mL | 1.9222 mL | |
| 40 mM | 0.0577 mL | 0.2883 mL | 0.5767 mL | 1.4417 mL | |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4613 mL | 1.1533 mL | |
| 60 mM | 0.0384 mL | 0.1922 mL | 0.3844 mL | 0.9611 mL | |
| 80 mM | 0.0288 mL | 0.1442 mL | 0.2883 mL | 0.7208 mL | |
| 100 mM | 0.0231 mL | 0.1153 mL | 0.2307 mL | 0.5767 mL |
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