product name NSC 405020
Description: NSC 405020 is a novel, noncatalytic small molecule inhibitor of MT1-MMP, it directly interacts with PEX domain of MT1-MMP and affects PEX homodimerization but has not catalytic activity of MT1-MMP. Inhibition of MT1-MMP expression by NSC405020 resulted in decrease of arsenic-mediated invasion of HSC5 cells involving decrease in phosphorylated extracellular signal-regulated kinases (pERK).
References: Cancer Res. 2012 May 1;72(9):2339-49.
260.16
Formula
C12H15Cl2NO
CAS No.
7497-07-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 52 mg/mL (199.9 mM)
Water: <1 mg/mL
Ethanol: 52 mg/mL (199.9 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 5 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: 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 Assay: 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 | 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. |
| Animal model | BALB/c nu/nu mice injected with MCF7-β3/WT and MCF7-β3/ΔPEX cells |
| Formulation & Dosage | Dissolved in 2% DMSO; 0.5 mg/kg; Intratumoral injection |
| References | Cancer Res. 2012 May 1;72(9):2339-49. |
