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NSC 405020

Catalog No.S8072

For research use only.

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.

CAS No. 7497-07-6

Selleck's NSC 405020 has been cited by 4 Publications

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MMP Signaling Pathway Map

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

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]

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]

Protocol (from reference)

Kinase Assay:^[1]	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:^[1]	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.
Animal Research:^[1]	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

References	[1] Remacle GG, et al. Cancer Res, 2012, 72(9), 2339-49.

References

[1] Remacle GG, et al. Cancer Res, 2012, 72(9), 2339-49.

Solubility (25°C)

In vitro	DMSO	52 mg/mL (199.87 mM)
	Ethanol	52 mg/mL (199.87 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 1% DMSO+30% polyethylene glycol+1% Tween 80 For best results, use promptly after mixing. Click to purchase: Tween 80	5 mg/mL

Chemical Information

Molecular Weight	260.16
Formula	C₁₂H₁₅Cl₂NO
CAS No.	7497-07-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCCC(C)NC(=O)C1=CC(=C(C=C1)Cl)Cl

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In vivo Formulation Calculator (Clear solution)

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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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