2. Metabolic Enzyme/Protease Apoptosis
  3. MMP Caspase Apoptosis
  4. MMP-9-IN-14

MMP-9-IN-14 是一种 MMP-9 抑制剂 (IC50 = 34.46 μM)。MMP-9-IN-14 可诱导癌细胞发生 G1 期细胞周期阻滞和 caspase 依赖性细胞凋亡 (apoptosis)。MMP-9-IN-14 可促进磷酸化 γH2AX 的积累。MMP-9-IN-14 可抑制癌细胞的迁移和侵袭，下调癌细胞中 MMP-2、MMP-9 和 hTERT 的表达。MMP-9-IN-14 可在动物模型中抑制肿瘤生长及血管趋向性扩散。MMP-9-IN-14 可用于肺腺癌、宫颈癌、结直肠癌等癌症的研究。

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MMP-9-IN-14

MMP-9-IN-14 Chemical Structure

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MMP-9-IN-14 相关抗体

Top Publications Citing Use of Products

查看 MMP 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MMP-9-IN-14 is a MMP-9 inhibitor (IC50 = 34.46 μM). MMP-9-IN-14 induces G1-phase cell cycle arrest and caspase-dependent apoptosis in cancer cells. MMP-9-IN-14 promotes the accumulation of phosphorylated γH2AX. MMP-9-IN-14 inhibits the migration and invasion of cancer cells, and downregulates the expressions of MMP-2, MMP-9 and hTERT in cancer cells. MMP-9-IN-14 inhibits tumor growth and angiogenic spread in animal models. MMP-9-IN-14 can be used for the research of cancers such as lung adenocarcinoma, cervical cancer and colorectal cancer[1].

IC50 & Target

MMP-9

34.46 μM (IC50)

Caspase 3

 

Caspase-7

 

MMP-2

 

体外研究
(In Vitro)


MMP-9-IN-14 (Compound 24) (0.39-100 μM; 30 min, 37°C) 可直接抑制重组人 MMP-9 酶活性，其 IC50 为 34.46 μM[1]。

MMP-9-IN-14 (0-50 μM；72 h) 抑制多种细胞系 (A-549，H-226，H-460，HCT-116，Hep G2，HeLa，HaCaT , MRC-5) 的活力，IC50 值分别为 2.23，2.34,，5.49，4.95，51.41，2.75，8.89，18.47 μM[1]。
MMP-9-IN-14 (2.23 μM; 24-72 h) 可在 A-549 细胞中诱导 G1 期细胞周期阻滞[1]。
MMP-9-IN-14 (2.23 μM; 24-72 h) 可诱导 A-549 细胞发生 caspase 依赖性细胞凋亡[1]。
MMP-9-IN-14 (2.23 μM; 24-72 h) 在 A-549 细胞中增加 γH2AX 阳性细胞数量，累积 DNA 损伤[1]。
Compound 24 (5-30 μM; 0-24 h) 抑制 A-549 癌细胞的迁移和侵袭[1]。
Compound 24 (15-30 μM; 48 h) 下调 A-549 细胞中转移相关基因 (MMP-2, MMP-9) 和 hTERT 的表达，并能强效抑制 TGF-β1 诱导的 MMP 表达[1]。
Compound 24 (10-50 μM; 72 h) 抑制 A-549 3D 球状体的增殖，在具有生理相关性的 3D 模型中展现出抗转移活性[1]。

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

MMP-9-IN-14 相关抗体:

Cell Viability Assay[1]

Cell Line: A-549，H-226，H-460，HCT-116，Hep G2，HeLa，HaCaT , MRC-5 cells
Concentration: 0-50 μM
Incubation Time: 72 h
Result: Inhibited the viability of various cell lines (A-549, H-226, H-460, HCT-116, Hep G2, HeLa, HaCaT, MRC-5), with IC50 values of 2.23, 2.34, 5.49, 4.95, 51.41, 2.75, 8.89, and 18.47, respectively.

Cell Cycle Analysis[1]

Cell Line: A-549 cells
Concentration: 2.23 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Caused a significant decrease in the S-phase population after 24 h treatment. Induced cell accumulation in the G1 phase with a reduction in G2/M content by 48 h treatment.
Induced a marked G1-phase arrest, with ~65% of cells in G1 phase and concurrent reductions in S and G2/M fractions at 72 h treatment.

Apoptosis Analysis[1]

Cell Line: A-549 cells
Concentration: 2.23 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Caused a increase in apoptosis, with ~10% early apoptotic and ~8% late apoptotic cells after 24 h treatment.
Increased early apoptosis to ~11% and late apoptosis to ~15%, with ~70% cell viability remaining at 48 h treatment.
Increased caspase-3/7 activity by ~5-fold at 24 h, ~5-6-fold at 48 h, and ~7-fold at 72 h compared to controls.

Cell Migration Assay [1]

Cell Line: A-549 cells
Concentration: 5, 10, 15 μM
Incubation Time: 0 h, 6 h, 12 h,
18 h, 24 h
Result: Significantly and in a concentration-dependent manner inhibited cell migration and delayed wound closure.

Cell Invasion Assay[1]

Cell Line: A-549 cells
Concentration: 15, 30 μM
Incubation Time: 24 h
Result: Reduced the number of invading A-549 cells to ~65% of control levels at 15 μM. Reduced the number of invading cells to ~25% of control levelsat 30 μM.

Real Time qPCR[1]

Cell Line: A-549 cells (with or without TGF-β1 stimulation)
Concentration: 15, 30 μM
Incubation Time: 48 h
Result: Significantly suppressed TGF-β1-induced MMP-2 and MMP-9 mRNA expression: at 15 μM, MMP-2 expression was reduced by ~60% and MMP-9 by ~70% ; at 30 μM, both MMP-2 and MMP-9 mRNA levels were reduced to near baseline. Downregulated hTERT expression: at 15 μM, hTERT expression was reduced by ~50%, and at 30 μM, was almost undetectable.
体内研究
(In Vivo)

MMP-9-IN-14 (compound 24) (25-50 μM; 局部给药；单次给药) 可抑制鸡胚尿囊膜 (CAM) 上 A-549 肿瘤生长，并可完全抑制肿瘤细胞的血管趋向性播散，且未检测到胚胎毒性[1]。

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

Animal Model: A-549 Xenotransplantation chorioallantoic membrane (CAM) model[1]
Dosage: 25 μM; 50 μM
Administration: topical; single administration
Result: Reduced median tumour area. Showed weaker, less homogeneous CellTracker Green signals in treated tumours, indicating reduced tumour cell viability/density.
Revealed a near-complete absence of disseminated fluorescent tumour cells in distal CAM regions, compared to frequent vasculotropic spread in vehicle controls.
分子量

481.39

Formula

C25H18Cl2N2O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MMP-9-IN-14 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

MMP-9-IN-14MMPCaspaseApoptosisMatrix metalloproteinasesMMP inhibitorapoptosischick chorioallantoic membrane (CAM)lung adenocarcinomacervical cancerlung cancer cellscolorectal cancerInhibitorinhibitorinhibit

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