2. Neuronal Signaling Stem Cell/Wnt Metabolic Enzyme/Protease Apoptosis
  3. Notch Phosphatase Apoptosis
  4. ZLDI-8

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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ZLDI-8 Chemical Structure

ZLDI-8 Chemical Structure

CAS No. : 667880-38-8

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Based on 1 publication(s) in Google Scholar

ZLDI-8 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ZLDI-8

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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 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[1][2].

IC50 & Target

ADAM-17[1]
IC50: 31.6 μM (Tyrosine phosphatase)[1]
Ki: 26.22 μM (Tyrosine phosphatase)[1]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZLDI-8 Related Antibodies

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].

MedChemExpress (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.
Molecular Weight

433.52

Formula

C24H23N3O3S
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
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
View the 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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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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ZLDI-8 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZLDI-8667880-38-8ZLDI8ZLDI 8NotchPhosphataseApoptosisADAM-17pithelial-mesenchymaltransitionanti-tumorNICDSurvivincIAP1/2N-CadherinVimentinE-CadherinSorafenibInhibitorinhibitorinhibit

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