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质量水平
检测方案
≥94% (HPLC)
形式
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
2-8°C
一般描述
一种细胞可渗透的三取代吡唑化合物，可作为有效和特异性整联蛋白连接激酶（ILK）抑制剂（IC50=600 nM）。显示对前列腺和乳腺癌细胞系具有高体外抗增殖效价（IC50 = 1 - 2.5 µM），同时保留正常上皮细胞。 其对癌症细胞的效应已归因于自噬和诱导的凋亡。抑制ILK介导的Ser473位点Akt磷酸化，从而下调下游靶标，如GSK-3b和肌球蛋白轻链。还引起转录因子Y-Box结合蛋白1（YB-1）的转录抑制。在小鼠模型中表现出最小毒性。
一种细胞可渗透的三取代吡唑化合物，可作为有效和特异性整联蛋白连接激酶（ILK）抑制剂（IC50=600 nM）。显示对前列腺和乳腺癌细胞系具有高体外抗增殖效价（IC50 = 1 - 2.5 M），同时保留正常上皮细胞。 其对癌症细胞的效应已归因于自噬和诱导的凋亡。抑制ILK介导的Ser473位点Akt磷酸化，从而下调下游靶标，如GSK-3b和肌球蛋白轻链。还引起转录因子Y-Box结合蛋白1（YB-1）的转录抑制。在小鼠模型中表现出最小毒性。
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多3个月。
其他说明
Lee, S., et al. 2011.J. Med. Chem.54, 6364
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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