2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Apoptosis
  3. HDAC ADAMTS Apoptosis Bcl-2 Family Cyclin G-associated Kinase (GAK)
  4. 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.

ZSNI-21

ZSNI-21 Chemical Structure

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ZSNI-21 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

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[1].

IC50 & Target[1]

HDAC2

0.844 μM (IC50)

HDAC6

0.106 μM (IC50)

HDAC1

1.270 μM (IC50)

Bax

 

Bcl-2

 

In Vitro

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.

ZSNI-21 Related Antibodies

Western Blot Analysis[1]

Cell Line: human hepatocellular carcinoma Bel-7402 cells
Concentration: 1.5 μM; 3 μM; 6 μM; 12 μM
Incubation Time: 48 h
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.

Cell Proliferation Assay[1]

Cell Line: human hepatocellular carcinoma Bel-7402 cells
Concentration: 3 μM; 6 μM; 12 μM
Incubation Time: 24 h
Result: Significantly reduced colony formation of Bel-7402 cells in a concentration-dependent manner, with colony formation rates decreasing notably at higher concentrations.

Apoptosis Analysis[1]

Cell Line: human hepatocellular carcinoma Bel-7402 cells
Concentration: 1.5 μM; 3 μM; 6 μM; 12 μM
Incubation Time: 48 h
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.

Cell Migration Assay [1]

Cell Line: human highly invasive hepatocellular carcinoma HCC-LM3 cells
Concentration: 1.5 μM; 3 μM; 6 μM
Incubation Time: 48 h
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.
In Vivo

ZSNI-21 (2000 mg/kg; i.g.; single dose) demonstrates high in vivo safety at a single 2000 mg/kg intragastric dose in C57BL/6 mice, with no observed mortality, weight loss, or organ pathology over 14 days[1].

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

Animal Model: C57BL/6 (female and male)[1]
Dosage: 2000 mg/kg
Administration: i.g.; single dose; 14-day observation
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.
Molecular Weight

459.49

Formula

C26H25N3O5
SMILES

COC(C=C1)=CC=C1OCCN2C(C)=C(C(NC3=CC=C(C(NO)=O)C=C3)=O)C4=C2C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ZSNI-21 Related Classifications

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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:

ZSNI-21ZSNI21ZSNI 21HDACADAMTSApoptosisBcl-2 FamilyCyclin G-associated Kinase (GAK)Histone deacetylasesAdamalysin-like metalloproteinase with thrombospondin motifsAuxilin 2HEK 293 Thepatocellular carcinomaMCF-7A549RBEHCC-LM3ADAM17Bel-7402HL-7702HDAC2Inhibitorinhibitorinhibit

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