SML0172
Cercosporamide from Cercosporidium henningsii
≥98% (HPLC)
Sinónimos:
4-Dibenzofurancarboxamide
Iniciar sesiónpara Ver la Fijación de precios por contrato y de la organización
About This Item
Fórmula empírica (notación de Hill):
C16H13NO7
Número de CAS:
Peso molecular:
331.28
UNSPSC Code:
12352200
NACRES:
NA.77
Productos recomendados
Quality Level
assay
≥98% (HPLC)
solubility
chloroform: 1 mg/mL
ethyl acetate: 1 mg/mL
DMSO: 5 mg/mL (Solution in DMSO is unstable and thus should be freshly prepared.)
storage temp.
−20°C
InChI
1S/C16H13NO7/c1-5(18)10-7(20)4-9-16(2,14(10)22)12-8(21)3-6(19)11(15(17)23)13(12)24-9/h3-4,19-21H,1-2H3,(H2,17,23)/t16-/m1/s1
InChI key
GEWLYFZWVLXQME-MRXNPFEDSA-N
Application
Cercosporamide from Cercosporidium henningsii has been used as a mitogen-activated protein (MAP) kinase-interacting kinase (MNK) inhibitor in glioblastoma (GBM)-derived BS287 spheres. It has also been used as an inhibitor of bone morphogenetic protein receptor (BMPR) type I kinase in HepG2 cells and zebrafish embryos in particular to test its rescue potential against developmental defects.
Biochem/physiol Actions
Cercosporamide was initially identified as a phytotoxin with broad-spectrum anti-fungal activity. Studies have shown that cercosporamide is a specific, highly potent fungal inhibitor of the cell wall integrity-signaling pathway mediator, protein kinase (Pkc1) inhibitor. Semisynthetic cercosporamide analogues demonstrated hypoglycemic activity and therefore, serve as candidates for potential new anti diabetic drugs. Cercosporamide was found to block eIF4E (Eukaryotic Initiation Factor) phosphorylation in cultured cancer cells, inducing apoptosis, suppressing proliferation, and reducing soft agar colonization. Its eIF4E phosphorylation inhibitory effect was also shown when administrated orally on xenograft human tissue and mouse liver tissue. Cercosporamide is a potent and selective Mnk inhibitor. It reduces tumor growth in xenografted HCT116 tumor and suppresses the outgrowth of B16 melanoma lung metastases. Hence, blocking Mnk function and eIF4E phosphorylation may be an attractive anticancer strategy.
Preparation Note
DMSO solution (1 mg/ml), kept at -20 °C, is stable for at least three months.
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
¿Ya tiene este producto?
Encuentre la documentación para los productos que ha comprado recientemente en la Biblioteca de documentos.
Li-Wei Wang et al.
Applied microbiology and biotechnology, 93(3), 1231-1239 (2011-08-05)
Through bioassay-guided fractionation, the EtOAc extract of a culture broth of the endophytic fungus Phoma species ZJWCF006 in Arisaema erubescens afforded a new α-tetralone derivative, (3S)-3,6,7-trihydroxy-α-tetralone (1), together with cercosporamide (2), β-sitosterol (3), and trichodermin (4). The structures of compounds
Kenji Wakabayashi et al.
Biological & pharmaceutical bulletin, 34(7), 1094-1104 (2011-07-02)
Peroxisome proliferator-activated receptor γ (PPARγ; NR1C3) is known as a key regulator of adipocytogenesis and the molecular target of thiazolidinediones (TZDs), also known as antidiabetic agents. Despite the clinical benefits of TZDs, their use is often associated with adverse effects
Akihiro Furukawa et al.
Bioorganic & medicinal chemistry letters, 20(7), 2095-2098 (2010-03-12)
In an investigation of (-)-Cercosporamide derivatives with a plasma glucose-lowering effect, we found that N-benzylcarboxamide derivative 4 was a partial agonist of PPARgamma. A SAR study of the substituents on carboxamide nitrogen afforded the N-(1-naphthyl)methylcarboxamide derivative 23 as the most
Jessica K Altman et al.
Blood, 121(18), 3675-3681 (2013-03-20)
Mnk kinases regulate the phosphorylation and activation of the eukaryotic initiation factor 4E (eIF4E), a protein that plays key roles in the initiation of messenger RNA translation and whose activity is critical for various cellular functions. eIF4E is deregulated in
Akihiro Furukawa et al.
European journal of medicinal chemistry, 54, 522-533 (2012-06-26)
Selective peroxisome proliferator-activated receptor gamma (PPARγ) modulators are expected to be a novel class of drugs improving plasma glucose levels without PPARγ-related adverse effects. As a continuation of our studies for (-)-Cercosporamide derivatives as selective PPARγ modulators, we synthesized substituted
Nuestro equipo de científicos tiene experiencia en todas las áreas de investigación: Ciencias de la vida, Ciencia de los materiales, Síntesis química, Cromatografía, Analítica y muchas otras.
Póngase en contacto con el Servicio técnico