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

ZLDI-8 

Cat. No.: HY-123931
Handling Instructions

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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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].

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].

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.

667880-38-8

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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

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

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