A cell-permeable, peptide-based (Z- QVPL) irreversible inhibitor of transglutaminase 2 (TG2) (IC50 = 150 nM for recombinant TG2) that acts by reacting with the active site cysteine of TG2. Exhibits far less potency against TG1 and TG3. Shown to significantly increase PGC-1a and cytochrome c mRNA levels in Q7 and Q111 cells (~50 mM). Also shown to enhance cytochrome c promoter activity by 250% in Q111 cells. Exhibits protective effect in cells exposed to 3-nitropropionic acid and NMDA, however, it does not directly affect mitochondrial bioenergetics.
Synonyms: Transglutaminase 2 Inhibitor, ZDON - Calbiochem; Z-DON, 6-diazo-5-oxo-norleucine tetrapeptide, TG2 Inhibitor
Molecular Formula: C31H45N7O9
Molecular Weight: 659.73
Linear Structural Formula: C31H45N7O9
Purity: >=98% (HPLC)
Legal Information: CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes: McConoughey, S. J., et al. 2010. EMBO Mol. Medicine.2, 349.