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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.
Yagishita, N., et al. 2012. Int. J. Mol. Med.30, 1281. Fujita, F., et al. 2015. EMBO J.34, 12192.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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).
Form
Purple solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₄H₃₆N₈O
Purity
≥97% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Yagishita, N., et al. 2012. Int. J. Mol. Med.30, 1281. Fujita, F., et al. 2015. EMBO J.34, 12192.
