553400

Radicicol, Diheterospora chlamydosporia

• Synonim(y): Radicicol, Diheterospora chlamydosporia
• Wzór empiryczny (zapis Hilla): C₁₈H₁₇ClO₆
• Numer CAS: 12772-57-5
• Masa cząsteczkowa: 364.78
• Numer MDL: MFCD06795865
• Kod UNSPSC: 51111800
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Formularz: solid
• siła działania: 0.27 nM IC₅₀
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 10 mg/mL; methanol: soluble
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• InChI: 1S/C18H17ClO6/c1-9-6-15-14(25-15)5-3-2-4-10(20)7-11-16(18(23)24-9)12(21)8-13(22)17(11)19/h2-5,8-9,14-15,21-22H,6-7H2,1H3/b4-2+,5-3+
• Klucz InChI: WYZWZEOGROVVHK-ZUVMSYQZSA-N

Opis

Opis ogólny

A cell-permeable, ATP-site binding, and irreversible antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60^v-src kinase activity (IC₅₀ = 0.27 nM). Inhibits the expression of COX-2 (IC₅₀ = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. Disrupts K-Ras-activated signaling pathways by selectively depleting Raf kinase. Inhibits tyrosine phosphorylation of p53/56^lyn in LPS-stimulated macrophages. Suppresses NIH/3T3 cell transformation by diverse oncogenes such as src, ras, and mos in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Also exhibits anti-angiogenic activity in vivo. Inhibits Wnt-5A expression in dermal papilla cells (IC₅₀ = 190 nM).

A cell-permeable, ATP-site binding, and irreversible antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60^v-src kinase activity (IC₅₀ = 0.27 µM). Inhibits the expression of COX-2 (IC₅₀ = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. Disrupts k-Ras-activated signaling pathway by selectively depleting Raf kinase. Inhibits tyrosine phosphorylation of p53/56^lyn in LPS-stimulated macrophages. Suppresses NIH 3T3 cell transformation by diverse oncogenes, such as src, ras and mos, at least in part by blocking the key signal transduction intermediates, such as MAP kinase and GAP-associated p62. Also exhibits anti-angiogenic activity in vivo. Inhibits Wnt-5A expression in dermal papilla cells (IC₅₀ = 190 nM).

Działania biochem./fizjol.

Primary Target
p60^v-src kinase activity

Secondary Target
COX-2 (IC₅₀ = 27 nM)

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Harmful (C)

Inne uwagi

Shinonaga, H., et al. 2009. Bioorg. Med. Chem.17, In press.
Soga, S., et al. 1998. J. Biol. Chem. 273, 822.
Chanmugam, P., et al. 1995. J. Biol. Chem. 270, 5418.
Shimada, Y., et al. 1995. J. Antibiot. 48, 824.
Zhao, J.F., et al. 1995. Oncogene 11, 161.
Oikawa, T., et al. 1993. Eur. J. Pharmacol. 241, 221.
Kwon, H.J., et al. 1992. Cancer Res. 52, 6926.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS06
• Hasło ostrzegawcze: Danger
• Zwroty wskazujące rodzaj zagrożenia: H301
• Zwroty wskazujące środki ostrożności: P264 - P270 - P301 + P310 - P405 - P501
• Klasyfikacja zagrożeń: Acute Tox. 3 Oral
• Kod klasy składowania: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable