Biochem/physiol Actions

Reversible: yes

Primary TargetSynoviolin

Cell permeable: yes

General description

A cell-permeable triaminotriazine that selectively inhibits the autoubiquitnation of the E3 ubiquitin ligase synoviolin (SYVN1, IC₅₀ = 35 µM), without affecting other E3 ubiquitin ligases. Abolished the SYVN-mediated negative regulation of PGC-1β via reduced ubiquitination. Shown to induce the expression of PGC-1β in wild type mouse embryonic fibroblasts (MEF), but does not affect PGC-1β expression in SYVN knockout MEFs. Increases mitochondrial biogenesis in C57BL/6J mice. Also increases the energy expenditure and causes a significant reduction in body weight and blood glucose levels in db/db mice (50 mg/kg, i.p daily) without influencing their food intake. Suppresses the proliferation of rheumatoid synovial cells (IC₅₀ = 5.4 µM) and reduces the severity of rheumatoid arthritis in a mouse model (4 mg/kg).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A cell-permeable triaminotriazine that selectively inhibits the autoubiquitnation of the E3 ubiquitin ligase synoviolin (SYVN1, IC₅₀ = 35 µM), without affecting other E3 ubiquitin ligases. Abolished the SYVN-mediated negative regulation of PGC-1β via reduced ubiquitination. Shown to induce the expression of PGC-1β in wild type mouse embryonic fibroblasts (MEF), but does not affect PGC-1β expression in SYVN knockout MEFs. Increases mitochondrial biogenesis in C57BL/6J mice. Also increases the energy expenditure and causes a significant reduction in body weight and blood glucose levels in db/db mice (50 mg/kg, i.p daily) without influencing their food intake. Suppresses the proliferation of rheumatoid synovial cells (IC₅₀ = 5.4 µM) and reduces the severity of rheumatoid arthritis in a mouse model (4 mg/kg).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Yagishita, N., et al. 2012. Int. J. Mol. Med.30, 1281.r>Fujita, F., et al. 2015. EMBO J.34, 12192.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)