TAPI-1

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
- 1. Zhang Y, Wang Y, et al. "Angiotensin Ⅱ deteriorates advanced atherosclerosis by promoting MerTK cleavage and impairing efferocytosis through AT1R/ROS/p38MAPK/ADAM17 pathway." Am J Physiol Cell Physiol. 2019 Aug 7. PMID:31390228
- 2. Zhou J, Sun J, et al. "MicroRNA-145 overexpression attenuates apoptosis and increases matrix synthesis in nucleus pulposus cells." Life Sci. 2019 Mar 15;221:274-283. PMID:30797016
- 3. Ellis-Connell AL, Balgeman AJ, et al. "ALT-803 transiently reduces SIV replication in the absence of antiretroviral treatment." J Virol. 2017 Nov 8. pii: JVI.01748-17. PMID:29118125
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 499.6 |
Cas No. | 171235-71-5 |
Formula | C26H37N5O5 |
Solubility | ≥24.98 mg/mL in DMSO; ≥15.77 mg/mL in EtOH with ultrasonic; ≥18.1 mg/mL in H2O |
Chemical Name | N1-((R)-1-(((R)-1-((2-aminoethyl)amino)-1-oxopropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide |
SDF | Download SDF |
Canonical SMILES | NCCNC([[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 Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
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. |
Description | TAPI-1 is an inhibitor of ADAM17/TACE. | |||||
Targets | ADAM17/TACE | |||||
IC50 |
Quality Control & MSDS
- View current batch:
Chemical structure

Related Biological Data

Related Biological Data

Related Biological Data
