579051

TAPI-1

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(s): TAPI-1, N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-1
• Empirical Formula (Hill Notation): C₂₆H₃₇N₅O₅
• CAS Number: 171235-71-5
• Molecular Weight: 499.60
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: methanol: 1 mg/mL; DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C26H37N5O5/c1-16(2)12-21(15-23(32)31-36)25(34)30-22(26(35)29-17(3)24(33)28-11-10-27)14-18-8-9-19-6-4-5-7-20(19)13-18/h4-9,13,16-17,21-22,36H,10-12,14-15,27H2,1-3H3,(H,28,33)(H,29,35)(H,30,34)(H,31,32)/t17-,21?,22-/m0/s1
• InChI key: AWNBSWDIOCXWJW-OWHMDLSXSA-N

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 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.

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).

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable