Inhibitor

MTG-Blocker



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Art. No. C102
Synonym BTG-Blocker
Background info Irreversible alkylation of the active site cysteine.
C102 has a molecular weight of about 510 Da and consists of an electrophilic warhead and a peptidic backbone. First, the MTGs active site cysteinyl residue attacks the warhead. A subsequent reaction leads to the release of a leaving group. Finally, the peptidic backbone is irreversibly attached to the MTG active site. As a consequence, the mass of the enzyme increases +482 Da due to the attached peptidic backbone.
Molecular Formula not disclosed
(Disclosure may be possible under a secrecy agreement)
Purity by HPLC >90 % (214 nm)
Appearance white solid
Solubility 2.5 mM in 0.5% (v/v) DMSO / aqueous buffers
Pre-dissolve e.g. 10 mg (19.6 μmol) in 39.2 μl DMSO - dilute e.g. 10 μl of that stock solution (500 mM) with 1990 μl aqueous buffer to obtain a 2.5 mM solution.
DMSO stock solutions are sterile and can be stored at -20°C for at least 6 months. To avoid too many freeze-thaw cycles, we strongly recommend storage of aliquots. Aqueous solutions are stable at room temperature for at least 3 days.
Reconstitution 500 μM in 0.1% (v/v) DMSO / aqueous buffers.
Pre-dissolve e.g. 10 mg (27 μmol) in 54 μl DMSO - dilute e.g. 5 μl of that stock solution (500 mM) with 4995 μl aqueous buffer to obtain a 500 μM solution.
Diluted buffer solutions must be consumed within 2 hours.
DMSO stock solutions can be stored at ambient temperature for 4 weeks.
Application Blocking of enzymatic activity of microbial (bacterial) transglutaminase IC50 ~ 125 μM
(Microbial Transglutaminase Assay Z009; Zedira, Germany)
Storage store at -20°C, desiccate
Reference(s) Rickert, M. et al. Protein Sci. 2016, 25, 442-455.
Spycher, P.R. et al. ChemBioChem 2017, 18, 1923-7.
Note INTENDED FOR RESEARCH USE ONLY, NOT FOR USE IN HUMAN, THERAPEUTIC OR DIAGNOSTIC APPLICATIONS.

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