Michael acceptor
peptidomimetics

Ac-(D)-Asp-MA-Nle-Nle-Leu-Pro-Trp-Pro-OH, "ZED1301"

Quantity Unit Price Status
5 mg 500 € Available
Documents
Art. No.
A108
Synonym
ZED1301
Background info
Peptidic inhibitor containing an electrophilic Michael acceptor (MA) warhead
Molecular Formula
C53H77N9O14
Molecular Weight
1064.23
Purity by HPLC
>95 % (214 nm)
Appearance
Off-white solid
Solubility
3.50 mg/ml (3.28 mM) in PBS buffer
Alternative 10 μM in 0.1% (v/v) DMSO / aqueous buffers
Pre-dissolve e.g. 2.15 mg (2.02 μmol) in 202 μl DMSO - dilute e.g. 10 μl of that stock solution (10 mM) with 9990 μl aqueous buffer to obtain a 10 μM solution. DMSO stock solutions can be stored at -20°C for at least 6 months. 
To avoid too many freeze-thaw cycles, we strongly recommend storage of aliquots.
Application
Site specific irreversible inhibitor of plasma transglutaminase (factor XIII, FXIII)
ZED1301 shows 30-fold selectivity for FXIII compared to tissue transglutaminase
IC50 = 100 nM (FXIII, using fluorescent Assay Substance A101[1])
IC50 = 3000 nM (TG2, using fluorescent Assay Substance A101[1])
[1] Oertel et al. Anal. Biochem. 2007, 367, 152.
Reference(s)
Stieler, M. et al. Angewandte Chemie Intl. Ed. 2013, 52, 11930.
Note
INTENDED FOR RESEARCH USE ONLY, NOT FOR USE IN HUMAN, THERAPEUTIC OR DIAGNOSTIC APPLICATIONS.

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