1. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis
  2. Microtubule/Tubulin MMP Apoptosis
  3. Tubulin/MMP-IN-2

Tubulin/MMP-IN-2 是微管蛋白和基质金属蛋白酶的双重抑制剂。Tubulin/MMP-IN-2 可强烈抑制微管蛋白聚合并诱导细胞凋亡。Tubulin/MMP-IN-2 对 MMP-2、MMP-3 和 MMP-9 具有抑制活性,IC50 值分别为 24.95 μM、31.60 μM 和 22.37 μM。Tubulin/MMP-IN-2 可用于癌症研究。

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Tubulin/MMP-IN-2 Chemical Structure

Tubulin/MMP-IN-2 Chemical Structure

CAS No. : 2734877-51-9

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  • 生物活性

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生物活性

Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer[1].

IC50 & Target

IC50: 0.36 μM (HepG-2), 0.31 μM (HT29), 0.19 μM (A549), 0.42 μM (MGC-803), 10.45 μM (LO2 cells); 0.32 μM (SK-OV-3), 0.39 μM (SK-OV-3/CDDP), 0.27 μM (MCF-7), 0.25 μM (MCF-7/DOX); 24.95 μM (MMP-2), 31.60 μM (MMP-3), 22.37 μM (MMP-9)[1].

体外研究
(In Vitro)

Tubulin/MMP-IN-2 (Compound 9e) (0.01-20 μM; 24 h) has activity for HepG-2, HT29, A549, MGC-803 and LO2 cells with IC50 values of 0.36 μM, 0.31 μM, 0.19 μM, 0.42 μM and 10.45 μM, respectively[1].
Tubulin/MMP-IN-2 has anti-proliferative activities for SK-OV-3, SK-OV-3/CDDP, MCF-7 and MCF-7/DOX cells with IC50 values of 0.32 μM, 0.39 μM, 0.27 μM and 0.25 μM, respectively[1].
Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively[1].
Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) strongly inhibits tubulin polymerization, and induced cell apoptosis and cell cycle arrest in G2/M stage, remarkably displayed inhibition of cell migration against A549 cells in vitro[1].
Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) can induce apoptosis via mitochondria-dependent apoptosis pathway[1].
Tubulin/MMP-IN-2 (2.5, 5 Μm; 24 h) can also cause ER stress demonstrating as up-regulation express of proteins (CHOP, p-elF2a, and p-PERK)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG-2, HT-29, A549, MGC-803, SK-OV-3, MCF-7, SK-OV-3/CDDP, MCF-7/DOX and normal liver cells LO2
Concentration: 0.01-20 μM
Incubation Time: 72 h
Result: Exhibited the most potent activity against various human cancer cells as well as multidrug-resistant tumor cells (A549/CDDP and MCF-7/DOX) and also showed significantly lower cytotoxic activity toward human normal liver cells LO2.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Significantly induced apoptosis after 24 h.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Induced a concentration-dependent G2/M stage arrest of A549 cells.

Immunofluorescence[1]

Cell Line: A549 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Remarkably induced changes in cell morphology, such as loss of membrane protrusions, disrupted microtubule organization and microtubule depolymerization, respectively.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Increased the accumulation of CHOP, p-eIF2a and p-PERK.
Promoted the expression of pro-apoptotic protein (Bax), and regulated down the level of anti-apoptotic protein (Bcl-2).
Increased the levels of caspase-3.
Lead p53 obviously up-regulated in a concentration-dependent manner.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Significantly reduced cell migration in a dose-dependent manner.
体内研究
(In Vivo)

Tubulin/MMP-IN-2 (15, 30 mg/kg; every two days for three weeks) displays significant in vivo antitumor efficacy in A549 xenograft models without inducing apparent systemic toxicity[1].

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

Animal Model: BALB/c nude mice[1]
Dosage: 15, 30 mg/kg
Administration: Every two days for three weeks
Result: Exhibited a dose-dependent inhibitory effect on tumor growth.
Exhibited no obvious histopathological changes for the main organ tissues (e.g. heart, liver, spleen, lung and kidney).
分子量

749.78

Formula

C40H48NO11P

CAS 号
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.

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参考文献
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  • 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.

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产品名称:
Tubulin/MMP-IN-2
目录号:
HY-152030
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