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Cat. No.: HY-152030

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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.

CAS No.: 2734877-51-9
Formula: C₄₀H₄₈NO₁₁P
Molecular Weight:749.78

Storage:

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

Data Sheet (275 KB)

Tubulin/MMP-IN-2 Chemical Structure

CAS No.: 2734877-51-9

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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].

All MMP Isoforms :

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]

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).

Chemical Information

CAS No. 2734877-51-9
Molecular Weight 749.78
Formula C₄₀H₄₈NO₁₁P
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xiaochao Huang, et al. Novel combretastatin A-4 derivative containing aminophosphonates as dual inhibitors of tubulin and matrix metalloproteinases for lung cancer treatment. Eur J Med Chem. 2022 Dec 15;244:114817. [Content Brief]

Calculators

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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

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Tubulin/MMP-IN-2

All MMP Isoforms