Inhibitor

MTG-Blocker



Order
Quantity
Price
Status
25 mg 385 € available


Documents
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.

Products

  • Zedira offers a huge portfolio of reliable specialist transglutaminase related products meant to catalyze research and development, both in academia and industry.

News  

  • imageReversibly acting transglutaminase 2 inhibitors: drug candidates for the treatment of fibrosis
  • Zedira supports Gordon Research Conference
  • imagePress release: Zedira announces ISO 9001:2015 certification
  • imageZedira communication: Joint poster presentation on “Feasibility of a new automated FXIII activity assay”
  • imageArtikel in DZG Aktuell 01/2019 über die klinische Wirksamkeitsstudie unseres potentiellen Zöliakie Medikaments (deutsch)
  • imagePreview: Catalogue Editorial 2019
  • Press release: Dr. Falk Pharma and Zedira announce start of the phase 2a proof of concept study of ZED1227 for the treatment of celiac disease
  • Artikel in DLG-Lebensmittel – 06/2017 zur Bestimmung von Transglutaminase in Lebensmitteln (deutsch)
  • Zedira publication: Microbial Transglutaminase Used in Bread Preparation at Standard Bakery Concentrations Does Not Increase Immunodetectable Amounts of Deamidated Gliadin
  • Pressemitteilung: Dr. Falk Pharma und Zedira geben den Abschluss der Phase 1b-Studie für ZED1227 zur Zöliakie-Therapie bekannt und planen Start der Wirksamkeitsstudie
  • Press release: Dr. Falk Pharma and Zedira announce completion of phase 1b clinical trial of ZED1227 for the treatment of celiac disease and move on to proof of concept study
  • Press Release: Dr. Falk Pharma GmbH and Zedira enter a phase 1b clinical trial for a celiac disease drug
  • Zedira publication: Microbial transglutaminase has a lower deamidation preference than human tissue transglutaminase on a celiac disease relevant wheat gliadin T-cell epitope
  • Press release: Additional subsidy funding for clinical development of a celiac disease drug
  • Pressemitteilung: Zusätzliche Fördermittel für die klinische Entwicklung eines Zöliakie-Medikamentes
  • Press Release: Cooperation between Zedira and Cardiff University - Transglutaminase 6 is the focus of new research into ataxia
  • Press Release: Dr. Falk Pharma and Zedira enter phase I clinical trials for a celiac disease drug
  • Press release: Zedira receives further funding to develop Factor XIIIa-blockers for safe anticoagulation

Blog  

Events  

  • 19th International Celiac Disease Symposium

    14.10.2021 - 17.10.2021
    Sorrento, Italy

  • Gordon Research Conference: Transglutaminases in Human Disease Processes

    12.06.2022 - 17.06.2022
    Mount Snow, USA