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化合物简介
Wortmannin, a steroid metabolite of the fungi Penicillium funiculosum, Talaromyces wortmannii, is a non-specific, covalent inhibitor of phosphoinositide 3-kinases (PI3Ks). It has an in vitro inhibitory concentration (IC50) of around 5 nM, making it a more potent inhibitor than LY294002, another commonly used PI3K inhibitor. It displays a similar potency in vitro for the class I, II, and III PI3K members although it can also inhibit other PI3K-related enzymes such as mTOR, DNA-PKcs, some phosphatidylinositol 4-kinases, myosin light chain kinase (MLCK) and mitogen-activated protein kinase (MAPK) at high concentrations , Wortmannin has also been reported to inhibit members of the polo-like kinase family with IC50 in the same range as for PI3K. The half-life of wortmannin in tissue culture is about 10 minutes due to the presence of the highly reactive C20 carbon that is also responsible for its ability to covalently inactivate PI3K. Wortmannin is a commonly used cell biology reagent that has been used previously in research to inhibit DNA repair, receptor-mediated endocytosis and cell proliferation.
基本信息
CAS:19545-26-7
中文别名:奥特曼宁;抗生素SL-2052;
英文别名:Wartmannin;SL-2052;Antibiotic SL-2052;
分子式:C23H24O8
分子量:428.432
精确质量:428.147
Psa:109.11
Logp:2.5364
中文别名:奥特曼宁;抗生素SL-2052;
英文别名:Wartmannin;SL-2052;Antibiotic SL-2052;
分子式:C23H24O8
分子量:428.432
精确质量:428.147
Psa:109.11
Logp:2.5364
编号系统
RTECS号:CB9641000
MDL号:MFCD00133927
EINECS号:214-538-0
BRN号:67676
PubChem号:24278777
MDL号:MFCD00133927
EINECS号:214-538-0
BRN号:67676
PubChem号:24278777
物化性质
外观与性状:白色固体
密度:1.39 g/cm3
沸点:615.6ºC at 760 mmHg
熔点:234-240ºC
闪点:326.1ºC
折射率:1.591
储存条件:2-8ºC
蒸汽压:4.35E-15mmHg at 25°C
密度:1.39 g/cm3
沸点:615.6ºC at 760 mmHg
熔点:234-240ºC
闪点:326.1ºC
折射率:1.591
储存条件:2-8ºC
蒸汽压:4.35E-15mmHg at 25°C
安全信息
安全说明:28-36/37-45
危险类别码:R26/27/28
危险品运输编码:UN 3462
危险品标志:T+
危险类别码:R26/27/28
危险品运输编码:UN 3462
危险品标志:T+
生产方法及用途
合成路线
-
参考文献
Sato, Seiji; Nakada, Masahisa; Shibasaki, Masakatsu Tetrahedron Letters, 1996 , vol. 37, # 34 p. 6141 - 6144
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