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NSC 405020

In stock
Catalog No.
A4051
MT1-MMP inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$66.00
In stock
10 mg
$60.00
In stock
50 mg
$230.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

NSC-405020 is a novel small molecule inhibitor of membrane type-I matrix metalloproteinase (MT1-MMP) that specifically targets the hemopexin (PEX) domain rather than the catalytic domain of MT1-MMP with 50% inhibition concentration IC50 value larger than 100 μmol/L and does not inhibit the catalytic activity of MT1-MMP or MMP-2. NSC-405020 directly interacts with and binds to PEX in a vicinity of Met-328, Arg-330, Asp-376, Met-22 and Ser-470 of the druggable pocket in the full-length MT1-MMP structure, which affects the conformation and flexibility of blades I to IV of the β-propeller resulting in the decrease of the PEX-dependent homodimerization of cellular MT1-MMP. NSC-405020 dose not affect the ability of MT1-MMP to activate MMP-2 but its ability to degrade COL-I.

Reference

Remacle AG, Golubkov VS, Shiryaev SA, Dahl R, Stebbins JL, Chernov AV, Cheltsov AV, Pellecchia M, Strongin AY. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012 May 1;72(9):2339-49. doi: 10.1158/0008-5472.CAN-11-4149. Epub 2012 Mar 9.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at RT
M.Wt260.16
Cas No.7497-07-6
FormulaC12H15Cl2NO
SynonymsNSC405020, NSC-405020
Solubility≥11.4 mg/mL in DMSO, ≥96.4 mg/mL in EtOH, <2.54 mg/mL in H2O
Chemical Name3,4-dichloro-N-pentan-2-ylbenzamide
SDFDownload SDF
Canonical SMILESCCCC(C)NC(=O)C1=CC(=C(C=C1)Cl)Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description NSC 405020 is a small-molecule inhibitor of Membrane type-1 matrix metalloproteinase (MT1-MMP) with IC50 value of > 100 μM.
Targets MT1-MMP          
IC50 > 100 μM          

Quality Control

Quality Control & MSDS

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Chemical structure

NSC 405020