NSC-405020|MT1-MMP inhibitor|DC Chemicals

Cas No.:	7497-07-6
Chemical Name:	3,4-Dichloro-N-(1-methylbutyl)benza-mide
Synonyms:	NSC405020,NSC-405020
SMILES:	C(NC(C)CCC)(=O)C1=CC=C(Cl)C(Cl)=C1
Formula:	C₁₂H₁₅Cl₂NO
M.Wt:	260.16
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

NSC-405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM 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.

Cat. No.	Product name	Field of application
DC72785	TP0597850	TP0597850 is a selective inhibitor of MMP2 (IC50=0.22 nM). TP0597850 has a long MMP2 dissociation half-life (t1/2=265 min).
DC8131	TAPI-2 (TNF Protease Inhibitor 2)	TAPI-2 inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 µM, respectively.
DC10713	S-methyl-KE-298	S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
DC7670	SB-3CT	SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively.
DC7215	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.
DC11404	JNJ0966	JNJ0966 is a highly selective compound that inhibited activation of MMP-9 zymogen and subsequent generation of catalytically active enzyme.
DC7135	GM6001 (galardin, ilomastat)	GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM.
DC10883	GI254023X	GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
DC11447	Astragaloside IV	Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.

NSC 405020