ZSNI-21
ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC50 0.939 μM and HDAC2 IC50 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C26H25N3O5
- Molecular Weight:459.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HDAC2 0.844 μM (IC50) |
HDAC6 0.106 μM (IC50) |
HDAC1 1.270 μM (IC50) |
Bax |
Bcl-2 |
ZSNI-21 (48 h) potently inhibits proliferation of Bel-7402, HCC-LM3, RBE, MCF-7, and A549 cancer cells with IC50 values ranging from 2.399 μM to 5.789 μM, while exhibiting low toxicity to HL-7702 and HEK 293 T normal cells[1].
ZSNI-21 functions as a dual inhibitor of ADAM17 and HDAC2 with IC50 values of 0.939 μM and 0.844 μM respectively, while also potently inhibiting HDAC6 (IC50 = 0.106 μM) and moderately inhibiting HDAC1 (IC50 = 1.270 μM)[1].
ZSNI-21 (6 h) exhibits strong intracellular binding affinity for ADAM17, HDAC1, HDAC2, and HDAC6 in Bel-7402 cells[1].
ZSNI-21 (1.5-12 μM; 48 h) reduces Notch intracellular domain (NICD) levels, increases acetylated histone H3 and H4 levels, modulates apoptosis-related proteins, and decreases Cyclin D1 expression in Bel-7402 cells[1].
ZSNI-21 (3-12 μM; 24 h) inhibits long-term proliferation and colony formation of Bel-7402 cells in a concentration-dependent manner[1].
ZSNI-21 (1.5-12 μM; 48 h) induces apoptosis in Bel-7402 cells in a concentration-dependent manner, as evidenced by apoptotic nuclear morphology and increased total apoptosis proportion (up to 40.2%)[1].
ZSNI-21 (1.5-6 μM; 48 h) inhibits migration of HCC-LM3 cells and reduces expression of EMT-related proteins in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human hepatocellular carcinoma Bel-7402 cells
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Concentration:1.5 μM; 3 μM; 6 μM; 12 μM
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Incubation Time:48 h
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Result:Significantly reduced NICD levels in a concentration-dependent manner (with stronger inhibition than ADAM17 inhibitor JG26).
Significantly increased levels of acetylated histones H3 and H4 (comparable to HDAC inhibitor SAHA).
Downregulated pro-caspase-3 expression in a concentration-dependent manner.
Downregulated Cyclin D1 expression in a concentration-dependent manner.
Downregulated Bcl-2 expression in a concentration-dependent manner.
Upregulated Bax expression in a concentration-dependent manner.
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Cell Line:human hepatocellular carcinoma Bel-7402 cells
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Concentration:3 μM; 6 μM; 12 μM
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Incubation Time:24 h
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Result:Significantly reduced colony formation of Bel-7402 cells in a concentration-dependent manner, with colony formation rates decreasing notably at higher concentrations.
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Cell Line:human hepatocellular carcinoma Bel-7402 cells
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Concentration:1.5 μM; 3 μM; 6 μM; 12 μM
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Incubation Time:48 h
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Result:Induced nuclear shrinkage and chromatin condensation (apoptotic features) in treated cells via Hoechst 33342 staining.
Increased total apoptosis proportion from 7% in controls to 15.83% to 40.2% in treated cells in a concentration-dependent manner via Annexin V-FITC/PI flow cytometry.
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Cell Line:human highly invasive hepatocellular carcinoma HCC-LM3 cells
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Concentration:1.5 μM; 3 μM; 6 μM
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Incubation Time:48 h
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Result:Significantly inhibited HCC-LM3 cell migration in a concentration-dependent manner via wound healing scratch assay.
Significantly reduced vimentin expression in a concentration-dependent manner via immunofluorescence and Western blot.
Significantly reduced Slug expression in a concentration-dependent manner via Western blot.
Significantly reduced MMP9 expression in a concentration-dependent manner via Western blot.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female and male)[1]
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Dosage:2000 mg/kg
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Administration:i.g.; single dose; 14-day observation
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Result:Showed no mortality over the 14-day period.
Showed no significant weight loss over the 14-day period.
Showed no significant pathological changes in heart, liver, spleen, lung, and kidney compared to controls.
Chemical Information
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Molecular Weight 459.49
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Formula C26H25N3O5
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SMILES
COC(C=C1)=CC=C1OCCN2C(C)=C(C(NC3=CC=C(C(NO)=O)C=C3)=O)C4=C2C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)