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

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.

For research use only. We do not sell to patients.

Tubulin/MMP-IN-2 Chemical Structure

Tubulin/MMP-IN-2 Chemical Structure

CAS No. : 2734877-51-9

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Description

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].

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].

MedChemExpress (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.
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].

MedChemExpress (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).
Molecular Weight

749.78

Formula

C40H48NO11P

CAS No.
SMILES

CCOP(OCC)(C(C1=CC=C(C=C1)OC)NC2=CC=C(C=C2)CC(OCCOC3=CC(/C=C\C4=CC(OC)=C(C(OC)=C4)OC)=CC=C3OC)=O)=O

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

Purity & Documentation
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    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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Product Name:
Tubulin/MMP-IN-2
Cat. No.:
HY-152030
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