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Merck
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重要文件

124018

Sigma-Aldrich

Akt抑制剂VIII，同工酶选择性，Akti-1/2

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS 612847-09-3, is a cell-permeable, reversible inhibitor of Akt1/Akt2 (IC₅₀ = 58 nM, 210 nM, & 2.12 µM for Akt1, Akt2, and Akt3, respectively).

同義詞:

Akt抑制剂VIII，同工酶选择性，Akti-1/2

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About This Item

經驗公式（希爾表示法）:
C34H29N7O
CAS號碼:
612847-09-3
分子量：:
551.64
MDL號碼:
MFCD09026909
分類程式碼代碼:
12352200
NACRES:
NA.28

品質等級

200

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

SMILES 字串

N6(CCC(CC6)[n]7c8c(nc7O)cccc8)Cc1ccc(cc1)c2nc3c(nc2c5ccccc5)cc4[nH]cnc4c3

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
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.

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

分析證明 (COA)

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