推荐产品
品質等級
化驗
≥95% (HPLC)
形狀
liquid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
desiccated (hygroscopic)
protect from light
運輸包裝
wet ice
儲存溫度
−70°C
一般說明
Akt1/Akt2活性的细胞可渗透,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。
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
请参考特定浓度批号的标签。
警告
毒性:刺激性(B)
外觀
10 mM(1 mg/181 µl)Akt抑制剂VIII,同工酶选择性,Akti-1/2(目录号124018)在DMSO中的溶液。
重構
初次解冻后,分装冻存(-70°C)。
其他說明
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.
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
10 - Combustible liquids
水污染物質分類(WGK)
WGK 2
閃點(°F)
188.6 °F - closed cup - (Dimethylsulfoxide)
閃點(°C)
87 °C - closed cup - (Dimethylsulfoxide)
The Journal of biological chemistry, 295(45), 15292-15306 (2020-09-02)
Muscle atrophy is regulated by the balance between protein degradation and synthesis. FOXO1, a transcription factor, helps to determine this balance by activating pro-atrophic gene transcription when present in muscle fiber nuclei. Foxo1 nuclear efflux is promoted by AKT-mediated Foxo1
Autophagy, 19(1), 152-162 (2022-04-19)
Impaired degradation of the transcriptional coactivator YAP1 and IL6ST (interleukin 6 cytokine family signal transducer), two proteins deregulated in liver cancer, has been shown to promote tumor growth. Here, we demonstrate that YAP1 and IL6ST are novel substrates of chaperone-mediated
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