Home Proteases MMP inhibitor NSC 405020 For research use only.

NSC 405020

NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.

NSC 405020 Chemical Structure

NSC 405020 Chemical Structure

CAS No. 7497-07-6

Purity & Quality Control

Batch: S807201 DMSO]125 mg/mL]false]Ethanol]52 mg/mL]false]Water]Insoluble]false Purity: 99.07%
99.07

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Signaling Pathway

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MMP Signaling Pathway

Biological Activity

Description NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.
Targets
MT1-MMP [1]
In vitro
In vitro NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP. NSC 405020 affects PEX homodimerization but not catalytic activity of MT1-MMP. NSC 405020 (100μM) inhibits migration of cells with high level of MT1-MMP, with a reduction of migration efficiency by about 75%. NSC 405020 does not inhibit migration of cells with low level of MT1-MMP and does not inhibit cell adhesion on collagen.[1]
Kinase Assay Migration assays
Assays are conducted in wells of a 24-well, 8 μm pore size Transwell plate. A 6.5-mm insert membrane is coated with 0.1 mL COL-I (300 μg/mL in MEGM) and then air dried for 16 hours. The collagen coating is rehydrated for 1 hour in 0.2 mL MEGM. The inner chamber contains MEGM-10% FBS as a chemoattractant. The compounds (10–100 μmol/L) or DMSO (0.1%–1%) are added to both inner and outer chambers. Before plating in the outer chamber, cells (5×104) are coincubated for 20 minutes with the compounds or DMSO in MEGM. Cells are allowed to migrate for 16 to 18 hours. The cells remaining on the top surface of the membrane are removed with a cotton swab. The cells on the bottom surface of the membrane are fixed and stained (0.2% crystal violet). The incorporated dye is extracted with 1% SDS and the A570 is measured.
Cell Research Cell lines 184B5-MT and MCF7-β3/MT
Concentrations ~400 μM
Incubation Time 24 or 30 h
Method Assays are conducted in wells of a 96-well flat bottom, white wall plates. 184B5-MT and MCF7-β3/MT cells (5×104) are grown for 16 hours in MEGM-10% FBS and DMEM-10% FBS, respectively. 184B5-MT cells are replenished with fresh MEGM (0.1 mL per well) and incubated for an additional 24 hours in the presence of the compounds (100 μM) or vehicle (1% DMSO). MCF7-β3/MT cells are replenished with fresh DMEM-10% FBS (0.1 mL per well) and incubated for an additional 6 hours in the presence of the compounds (400 μM) or vehicle (2% DMSO). The viable cells are counted using a luminescent ATP-Lite assay.
In Vivo
In vivo NSC 405020 (0.5 mg/kg, intratumoral injection) significantly represses tumor growth. NSC 405020 causes a fibrotic, ΔPEX-like tumor phenotype and increases the level of COL-I. [1]
Animal Research Animal Models BALB/c nu/nu mice injected with MCF7-β3/WT and MCF7-β3/ΔPEX cells
Dosages 0.5 mg/kg, 3 times per week
Administration Intratumoral injection

Chemical Information & Solubility

Molecular Weight 260.16 Formula

C12H15Cl2NO
CAS No. 7497-07-6 SDF Download NSC 405020 SDF
Smiles CCCC(C)NC(=O)C1=CC(=C(C=C1)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 125 mg/mL ( (480.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 52 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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