2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis
  3. Microtubule/Tubulin MMP Apoptosis
  4. 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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Tubulin/MMP-IN-2 相关抗体

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.19 μM
Compound: 9e
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
HepG2 IC50
0.36 μM
Compound: 9e
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
HT-29 IC50
0.31 μM
Compound: 9e
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
L02 IC50
10.45 μM
Compound: 9e
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
MCF7 IC50
0.27 μM
Compound: 9e
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
MGC-803 IC50
0.42 μM
Compound: 9e
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
SK-OV-3 IC50
0.32 μM
Compound: 9e
Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 36252396]
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.

Tubulin/MMP-IN-2 相关抗体:

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.
纯度 & 产品资料
参考文献

Tubulin/MMP-IN-2 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tubulin/MMP-IN-22734877-51-9Microtubule/TubulinMMPApoptosisMatrix metalloproteinasesTubulinmatrix metalloproteinasesapoptosisMMP-2MMP-3MMP-9cancerInhibitorinhibitorinhibit

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