NSC 405020, inhibitor

NSC 405020

Cat. Num. AAA575642

• Purity: 97.0%
• Synonyms: NSC 405020; inhibitor

• Purity/Purification: 97.0%
• Form/Format: POWDER

• Solubility: DMSO: 26 mg/mL (100 mM); Ethanol: 26 mg/mL (100 mM); (< 1 mg/ml refers to the product slightly soluble or insoluble).
• CAS: 7497-07-6
• Formula: C12H15Cl2NO
• Target (IC50): MT1-MMP: None
• Kinase Assay: Migration assays: Assays are conducted in wells of a 24-well, 8 ?m pore size Transwell plate. A 6.5-mm insert membrane is coated with 0.1 mL COL-I (300 ?g/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 ?mol/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: Assays are conducted in wells of a 96-well flat bottom, white wall plates. 184B5-MT and MCF7-?3/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 ?M) or vehicle (1% DMSO). MCF7-?3/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 ?M) or vehicle (2% DMSO). The viable cells are counted using a luminescent ATP-Lite assay.(Only for Reference); Cell lines: 184B5-MT and MCF7-?3/MT
• 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 (100 ?M) 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.
• 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.
• Preparation and Storage: Store at -20 degree C.

Structure

Stock Solutions

(Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product in different solvents. The storage conditions and period of the stock solution: - 80°C for 6 months; -20°C for 1 month. Please use it as soon as possible.)

Related Product Information for NSC 405020, inhibitor

NSC 405020 is a noncatalytic inhibitor of MT1-MMP.