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製品番号: HY-187511

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NS06

NS06 is a dual-target inhibitor of STAT3 and HDAC, with a K_d 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 番号: 3133892-41-5
分子式: C₂₀H₂₂Cl₂N₄O₆
分子量:485.32

保管条件:

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

NS06 構造式

CAS 番号: 3133892-41-5

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

STAT3

5.82 μM (Kd)

hHDAC1

129.1 nM (IC₅₀)

hHDAC3

451.2 nM (IC₅₀)

hHDAC6

230.4 nM (IC₅₀)

STAT アイソフォーム固有の製品をすべて表示 :

HDAC アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	1.49 μM	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.	42526131
MCF7	IC50	1.99 μM	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.	42526131
HCT-116	IC50	1.41 μM	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.	42526131
SW-620	IC50	1.74 μM	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.	42526131
SGC-7901	IC50	6.40 μM	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.	42526131
BGC-823	IC50	4.28 μM	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.	42526131
NCM460	IC50	33.86 μM	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.	42526131

体外実験

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 (K_D = 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.

Western Blot Analysis^[1]

Cell Line:

Human HCT116 colon cancer cells, MDA-MB-231 breast cancer cells
Concentration:

1 μM
Incubation Time:

4 h
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.

Cell Proliferation Assay^[1]

Cell Line:

Human HCT116 colon cancer cells
Concentration:

1 μM
Incubation Time:

10 days (medium refreshed every 3 days)
Result:

Significantly reduced colony formation relative to the DMSO (Dimethyl sulfoxide) (HY-Y0320C) control.

Cell Migration Assay ^[1]

Cell Line:

Human HCT116 colon cancer cells
Concentration:

1 μM
Incubation Time:

48 h
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.

Apoptosis Analysis^[1]

Cell Line:

Human HCT116 colon cancer cells
Concentration:

1 μM; 2 μM
Incubation Time:

48 h
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.

Related Protocols :

化学情報

CAS 番号 3133892-41-5
分子量 485.32
分子式 C₂₀H₂₂Cl₂N₄O₆
SMILES

ONC(CCCCNCCOC1=CC=C(Cl)C=C1C(NC2=CC=C([N+]([O-])=O)C=C2Cl)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Shi Y, et al. Design, synthesis, and evaluation of anti-solid-tumor activity of niclosamide-based STAT3/HDAC dual-target inhibitors. Bioorganic chemistry. 2026 Jul 25;181:110272. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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NS06

STAT アイソフォーム固有の製品をすべて表示

HDAC アイソフォーム固有の製品をすべて表示