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TAPI-1

In stock
Catalog No.
B4686
TACE/ADAM17 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$780.00
In stock
1mg
$189.00
In stock
5mg
$662.00
In stock

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Background

TAPI-1 is an inhibitor of tumour necrosis factor with IC50 value of 8.09 μM [1].

TAPI-1 is an inhibitor of TACE/ADAM17 which catalyzes the cleavage of full-length APP to the soluble N-terminal fragment (sAPPα). The release of sAPPα has been reported to be a receptor-coupled process increased by the stimulation of muscarinic receptors. In HEK293 cells, treatment of TAPI-1 resulted in an inhibition of increased sAPPα which was induced by the expressing of M3 subtype. The IC50 values of TAPI-1 in the inhibition of M3-increased sAPPα and constitutive release of sAPPα were 3.61 μM and 8.09 μM, respectively. Besides APP, TAPI-1 was also found to have inhibitory effects on the release of TNF-α, IL6R, TNFRI and TNFRII with IC50 values of 50-100, 5-10, 5-10 and 25-50 mM, respectively [1, 2].

References:
[1] Slack B, Ma L, Seah C. Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme. Biochem. J, 2001, 357: 787-794.
[2] Hooper N, Karran E, Turner A. Membrane protein secretases. Biochem. J, 1997, 321: 265-279.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt499.6
Cas No.171235-71-5
FormulaC26H37N5O5
Solubility≥24.98mg/mL in DMSO
Chemical NameN1-((R)-1-(((R)-1-((2-aminoethyl)amino)-1-oxopropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide
SDFDownload SDF
Canonical SMILESNCCNC([[email protected]@H](C)NC([[email protected]](NC(C(CC(C)C)CC(NO)=O)=O)CC1=CC2=CC=CC=C2C=C1)=O)=O
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.

Protocol

Cell experiment:

Cell lines

human pulmonary mucoepidermoid carcinoma cell line, NCI-H292 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

30 min, 30 μM [1]

Applications

TAPI-1, tumor necrosis factor ɑ protease inhibitor-1, is an inhibitor of TACE (TNF-α converting enzyme). TAPI-1 inhibits ectodomain shedding of TNF-ɑ, L-selectin, and p55 TNF-ɑ receptor. Pretreating cells with TAPI-1 inhibits PMA-induced EGFR phosphorylation. Besides, TAPI-1 could block TGF-ɑ release and block the production of mucin induced by PMA, PA sup, and LPS [1]. TAPI-1 is also a general matrix metalloproteinase (MMP) and ADAM inhibitor [2].

References:

[1]. Shao MX, Ueki IF, Nadel JA. Tumor necrosis factor alpha-converting enzyme mediates MUC5AC mucin expression in cultured human airway epithelial cells. Proc Natl Acad Sci U S A. 2003 Sep 30;100(20):11618-23.

[2]. Chen CD, Podvin S, Gillespie E, Leeman SE, Abraham CR. Insulin stimulates the cleavage and release of the extracellular domain of Klotho by ADAM10 and ADAM17. Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19796-801.

Biological Activity

Description TAPI-1 is an inhibitor of ADAM17/TACE.
Targets ADAM17/TACE          
IC50            

Quality Control

Chemical structure

MLN9708

Related Biological Data

MLN9708

Related Biological Data

MLN9708