TAPI 0

Names

[ CAS No. ]:
163958-73-4

[ Name ]:
TAPI 0

[Synonym ]:
N-[(2R)-2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-(2-naphthalenyl)-L-alanyl-L-alaninamide
TAPI-0
TNF-α Protease Inhibitor-0
N-(R)-(2-(Hydroxyaminocarbonyl)Methyl)-4-Methylpentanoyl-L-Naphthylalanyl-L-Alanine amide
MFCD02684279
TNF-α Processing Inhibitor-0

Biological Activity

[Description]:

TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing[1][2].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Infection
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP
Signaling Pathways >> Anti-infection >> Bacterial

[Target]

IC50: 100 nM (TACE)[2]


[In Vitro]

TAPI-0 inhibits peptide deformylase (PDF) with an IC50 of 18 nM. TAPI-0 suppresses chlamydial growth by targeting the bacterial PDF[1].

[References]

[1]. Amit Balakrishnan, et al. Metalloprotease inhibitors GM6001 and TAPI-0 inhibit the obligate intracellular human pathogen Chlamydia trachomatis by targeting peptide deformylase of the bacterium. J Biol Chem. 2006 Jun 16;281(24):16691-9.

[2]. Shiori Haga, et al. TACE antagonists blocking ACE2 shedding caused by the spike protein of SARS-CoV are candidate antiviral compounds. Antiviral Res. 2010 Mar;85(3):551-5.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Molecular Formula ]:
C24H32N4O5

[ Molecular Weight ]:
456.53

[ Exact Mass ]:
456.237274

[ LogP ]:
1.31

[ Index of Refraction ]:
1.587

[ Water Solubility ]:
Soluble to 10 (mg/mL) in DMSO

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310 + P330

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds