[CAS NO. 667880-38-8] ZLDI-8
PRODUCTS SPECIFICATIONS [667880-38-8]
DESCRIPTION [667880-38-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 433.52 |
| Molecular Formula | C24H23N3O3S |
| SMILES | O=C(/C(C(N1)=O)=C/C2=C(C)N(CCOC3=CC=C(C)C=C3C)C4=C2C=CC=C4)NC1=S |
1 Publications Citing Use of MCE
Summary
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 [1] [2] .
IC50 & Target
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
[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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| 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 [1]
| 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 |
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Nude mice with MHCC-97H cells [1] |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 144.17 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3067 mL | 11.5335 mL | 23.0670 mL |
| 5 mM | 0.4613 mL | 2.3067 mL | 4.6134 mL |
| 10 mM | 0.2307 mL | 1.1533 mL | 2.3067 mL |
References
- [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.
- [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.
