检测方案
≥98% (HPLC)
质量水平
形式
solid
效能
0.27 nM IC50
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 10 mg/mL
methanol: soluble
运输
ambient
储存温度
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+
InChI key
WYZWZEOGROVVHK-ZUVMSYQZSA-N
一般描述
A cell-permeable, ATP-site binding, and irreversible antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60v-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 p53/56lyn 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 p60v-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 p53/56lyn 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).
生化/生理作用
Primary Target
p60v-src kinase activity
p60v-src kinase activity
Secondary Target
COX-2 (IC₅₀ = 27 nM)
COX-2 (IC₅₀ = 27 nM)
包装
Packaged under inert gas
警告
Toxicity: Harmful (C)
其他说明
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.
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
监管及禁止进口产品
Bingshe Han et al.
Frontiers in genetics, 11, 541944-541944 (2020-12-22)
Accumulating evidence indicates that heat shock protein 90 (HSP90) plays essential roles in modulation of phenotypic plasticity in vertebrate development, however, the roles of HSP90 in modulation of cold tolerance capacity in fish are still unclear. In the present study
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