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579051 Sigma-Aldrich

TAPI-1 - CAS 171235-71-5 - Calbiochem

TAPI-1, CAS 171235-71-5, is a structural analog of TAPI-0 with similar in vitro efficacy for the inhibition of MMPs and TACE. Blocks the shedding of several cell surface proteins.

Synonym: N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-1, TAPI-1 - CAS 171235-71-5 - Calbiochem

  • CAS Number 171235-71-5

  • Empirical Formula (Hill Notation) C26H37N5O5

  • Molecular Weight 499.60

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Properties

Related Categories A to C, Biochemicals and Reagents, Collagenase, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme,
Quality Level   100
assay   ≥97% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  desiccated
  protect from light
storage conditions   -20C
color   white
solubility   methanol: 1 mg/mL
  DMSO: 5 mg/mL
shipped in   ambient

Description

General description

A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α convertase; ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC50 = 8.09 µM) and muscarinic receptor-stimulated (IC50 = 3.61 µM) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC50 = 920 nM).

A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α converting enzyme/ADAM17). TAPI-1 also blocks the shedding of several cell surface proteins such as IL-6 receptor, p60 TNF receptor, and p80 TNF receptor. Blocks constitutive (IC50 = 8.09 µM) and muscarinic receptor-stimulated (IC50 = 3.61 µM) sAAPα release in HEK 293 cells expressing M3 muscarinic receptors. A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579050) in DMSO is also available.

Packaging

1 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: no

Primary Target
MMPs and TACE

Product does not compete with ATP.

Reversible: no

Target IC50: 8.09 µM and 3.61 µM blocking constitutive and muscarinic receptor-stimulated sAAPα release in HEK 293 cells expressing M3 muscarinic receptors, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Slack, B.E., et al. 2001. Biochem. J.357, 787.
Vincent, B., et al. 2001. J. Biol. Chem.276, 37743.
Hooper, N.M., et al. 1997. Biochem. J.321, 265.
Crowe, P.D., et al. 1995. J. Exp. Med.181, 1205.
Mullberg, J., et al. 1995. J. Immunol.155, 5198.
Mohler, K.M., et al. 1994. Nature370, 218.

Legal Information

Manufactured exclusively by Peptides International, Louisville, Kentucky, USA.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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