NS06
NS06 is a dual-target inhibitor of STAT3 and HDAC, with a Kd of 5.82 μM for human STAT3, an IC50 of 129.1 nM for human HDAC1, an IC50 of 451.2 nM for human HDAC3, and an IC50 of 230.4 nM for human HDAC6. NS06 binds to STAT3 to inhibit its phosphorylation without altering the total STAT3 level; it inhibits the enzymatic activity of HDAC via coordination with Zn2+ at the catalytic center of HDAC1 and increases the acetylation level of histone H3. NS06 induces cell apoptosis, inhibits cancer cell migration and colony formation, and exhibits antiproliferative activity against solid tumor cells and 3D tumor spheroid models. NS06 is applicable to solid tumor-related research.
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- CAS No.: 3133892-41-5
- Formule: C20H22Cl2N4O6
- Masse moléculaire:485.32
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
STAT3 5.82 μM (Kd) |
hHDAC1 129.1 nM (IC50) |
hHDAC3 451.2 nM (IC50) |
hHDAC6 230.4 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | IC50 |
1.49 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
| MCF7 | IC50 |
1.99 μM
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Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
| HCT-116 | IC50 |
1.41 μM
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Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
| SW-620 | IC50 |
1.74 μM
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Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
| SGC-7901 | IC50 |
6.40 μM
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Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
| BGC-823 | IC50 |
4.28 μM
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Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
| NCM460 | IC50 |
33.86 μM
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Antiproliferative activity against non-cancerous human NCM460 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against non-cancerous human NCM460 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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42526131 |
In Vitro
NS06 (30-60 min) potently inhibits recombinant human HDAC1 (IC50 = 129.1 nM), HDAC3 (IC50 = 451.2 nM), and HDAC6 (IC50 = 230.4 nM) in vitro, with limited activity against HDAC4 and HDAC11[1].
NS06 (0.31-10.0 μM) binds directly to recombinant human STAT3 protein with moderate affinity (KD = 5.82 μM) in vitro[1].
NS06 (5 μM; 0-150 min) shows moderate metabolic stability in rat liver microsomes, with a half-life of 48.6 min and an intrinsic clearance of 28.53 μL/min/mg microsomal protein[1].
NS06 (0.10-100 μM; 48 h) shows potent, selective antiproliferative activity against human solid-tumor cell lines (IC50 = 1.41-6.40 μM) with low cytotoxicity toward non-cancerous NCM460 cells (IC50 = 33.86 μM), resulting in favorable selectivity indices for most tumor cell lines[1].
NS06 (1 μM; 4 h) increases acetylated histone H3 levels in HCT116 and MDA-MB-231 cells, confirming functional intracellular HDAC inhibition[1].
NS06 (1 μM; 4 h) suppresses STAT3 phosphorylation in HCT116 and MDA-MB-231 cells without affecting total STAT3 protein levels[1].
NS06 (1 μM; 10 days) potently inhibits long-term colony formation in HCT116 cells[1].
NS06 (1 μM; 48 h) potently inhibits Transwell migration of HCT116 cells[1].
NS06 (1-2 μM; 29 days) inhibits 3D HCT116 tumor spheroid growth in a concentration-dependent manner[1].
NS06 (1-2 μM; 48 h) induces concentration-dependent apoptosis in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human HCT116 colon cancer cells, MDA-MB-231 breast cancer cells
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Concentration:1 μM
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Incubation Time:4 h
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Result:Increased acetylated histone H3 (Ac-H3) levels in both HCT116 and MDA-MB-231 cells to an extent comparable to the pan-HDAC inhibitor SAHA.\nReduced phosphorylated STAT3 (p-STAT3) levels in both HCT116 and MDA-MB-231 cells without altering total STAT3 expression.
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Cell Line:Human HCT116 colon cancer cells
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Concentration:1 μM
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Incubation Time:10 days (medium refreshed every 3 days)
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Result:Significantly reduced colony formation relative to the DMSO (Dimethyl sulfoxide) (HY-Y0320C) control.
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Cell Line:Human HCT116 colon cancer cells
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Concentration:1 μM
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Incubation Time:48 h
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Result:Reduced the number of migrated cells from 313 (DMSO control) to 90 (P < 0.001), with an inhibitory effect comparable to SAHA, niclosamide, and the niclosamide + SAHA combination.
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Cell Line:Human HCT116 colon cancer cells
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Concentration:1 μM; 2 μM
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Incubation Time:48 h
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Result:Increased the apoptotic fraction from 1.3% (DMSO control) to 28.4% at 1 μM.
Increased the apoptotic fraction further to 37.9% at 2 μM.
Showed stronger response than niclosamide or SAHA alone, and comparable to or exceeding the niclosamide + SAHA combination.
- Western Blot
- Scratch/Wound-Healing Migration Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Suspension Spheroid Formation (Low-Adhesion/Forced Aggregation)
- Hanging Drop Spheroid Culture
- Colony Formation (Clonogenic) Assay
- 3D Tumor Spheroid Invasion Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Chemotaxis Gradient Chamber Assay 1
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Apoptosis Solutions
- 3D Collagen/Hydrogel Matrix Migration Assay
- Protocol for Kinase activity and phosphorylation assays
- Soft Agar Colony Formation Assay
- Cell-Exclusion Zone Migration Assay
- Chemotaxis Gradient Chamber Assay 2
Chemical Information
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CAS No. 3133892-41-5
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Masse moléculaire 485.32
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Formule C20H22Cl2N4O6
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SMILES
ONC(CCCCNCCOC1=CC=C(Cl)C=C1C(NC2=CC=C([N+]([O-])=O)C=C2Cl)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NS06 Related Classifications
HY-187511 Related Classifications
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