5.38184

Synoviolin Inhibitor, LS-102

• Sinônimo(s): Synoviolin Inhibitor, LS-102, (S)-N²-(benzo[d]oxazol-6-yl)-N⁴-(1-cyclohexylethyl)-N⁶-ethyl-N⁶-(2-(ethylamino)ethyl)-1,3,5-triazine-2,4,6-triamine, E3 Ligase SYVN Inhibitor, LS-102, LS102
• Fórmula empírica (Notação de Hill): C₂₄H₃₆N₈O
• Peso molecular: 452.60
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥97% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• potência: 35 μM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: purple
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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).

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Synoviolin

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

Yagishita, N., et al. 2012. Int. J. Mol. Med.30, 1281.

Fujita, F., et al. 2015. EMBO J.34, 12192.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable