Factor XIII Inhibitor

Description
Ac-(D)-Asp-MA-Nle-Nle-Leu-Pro-Trp-Pro-OH is a site specific irreversible inhibitor of plasma trans-glutaminase (factor XIII, FXIII). Peptidic inhibitor containing an electrophilic Michael acceptor (MA) warhead.
The inhibitor 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⁾

Molecular Formula: C₅₃H₇₇N₉O₁₄                                               

Chemical Structure:


Molecular Weight: 1064.23

Purity by HPLC: >95 % (214 nm)

Presentation
5 mg off pale yellow solid powder

Solubility
3.50 mg/ml (3.28 mM) in PBS buffer.

Alternative 10μM 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 (10mM) 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.

Storage    
Store at -20°C, desiccate

Category: Research use only

Type: Inhibitor

Product Availability: Worldwide

Manufacturer: ImmBioMed GmbH & Co KG, Germany
 

References

1. A highly sensitive fluorometric assay for deter-mination of human coagulation factor XIII in plasma. Oertel K et al. Anal Biochem. 2007 Aug 15;367(2):152-158.
2. Structure of active coagulation factor XIII triggered by calcium binding: basis for the design of next-generation anticoagulants. Stieler M et al. Angew Chem Int Ed Engl. 2013 Nov 4;52(45):11930-4