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品質等級
化驗
≥95% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
yellow
溶解度
DMSO: 5 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
InChI
1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)
InChI 密鑰
BIWGYFZAEWGBAL-UHFFFAOYSA-N
一般說明
Akt1/Akt2活性的细胞可渗透，可逆，有效和选择性抑制剂（在体外激酶测定中，Akt1，Akt2和Akt3的IC50分别为58 nM，210 nM和2.12 µM）。据报道抑制作用具有普列克底物蛋白同源物（PH）域依赖性。即使在50 µM的高浓度情况下，它也不会对缺乏PH结构域的Akt或其他紧密相关的AGC家族激酶，PKA，PKC和SGK表现出任何抑制作用。克服了Akt1/Akt2介导的肿瘤细胞对化学疗法的抗性并显示出在体外培养的细胞和体内小鼠中均能阻断Akt1/Akt2的基础和刺激的磷酸化/激活。
一种可渗透细胞且可逆的喹喔啉化合物，可有效选择性地抑制Akt1/Akt2活性（在体外激酶测定中，Akt1，Akt2和Akt3的IC50分别为58 nM，210 nM和2.12 µM）。抑制作用似乎具有普列克底物蛋白同源物（PH）域依赖性。即使在50 µM的高浓度情况下，它也不会对缺乏PH结构域的Akt或其他紧密相关的AGC家族激酶，PKA，PKC和SGK表现出任何抑制作用。克服了Akt1/Akt2介导的肿瘤细胞对化学疗法的抗性并显示出在体外培养的细胞和体内小鼠中均能阻断Akt1/Akt2的基础和刺激的磷酸化/激活。也可获得10 mM（1 mg/181 µl）Akt抑制剂VIII，同工酶选择性，Akti-1/2（目录号124017）在DMSO中的溶液。
生化／生理作用
主要靶标
Akt1, Akt2, Akt3
Akt1, Akt2, Akt3
产物不与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：在体外激酶测定中，Akt1，Akt2和Akt3分别为58 nM，210 nM和2.12 µM
包裝
用惰性气体包装
警告
毒性：标准处理（A）
重構
在复溶后，分装并冷冻保存（-70°C）。储备液可在-70°C最长稳定6个月。
其他說明
Calleja, V., et al. 2009.PLoS Biol.7, e17.
Logie, L., et al. 2007.Diabetes56, 228.
Barnett, S.F., et al. 2005.Biochem.J.385, 399.
DeFeo-Jones, D., et al. 2005.Mol.Cancer Ther.4, 271.
Zhao, Z., et al. 2005.Bioorg.Med. Chem. Lett.15, 905.
Lindsley, C.W., et al. 2005.Bioorg.Med. Chem. Lett.15, 761.
Logie, L., et al. 2007.Diabetes56, 228.
Barnett, S.F., et al. 2005.Biochem.J.385, 399.
DeFeo-Jones, D., et al. 2005.Mol.Cancer Ther.4, 271.
Zhao, Z., et al. 2005.Bioorg.Med. Chem. Lett.15, 905.
Lindsley, C.W., et al. 2005.Bioorg.Med. Chem. Lett.15, 761.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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