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Merck
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文件

124020

Sigma-Aldrich

Akt抑制剂X

The Akt Inhibitor X, also referenced under CAS 925681-41-0, controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

Akt抑制剂X, 10-(4ʹ-(N-二乙氨基)丁基)-2-氯吩恶嗪,HCl,10-NCP

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About This Item

经验公式(希尔记法):
C20H25ClN2O · xHCl
分子量:
344.88 (free base basis)
分類程式碼代碼:
12352200
NACRES:
NA.77

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
desiccated (hygroscopic)
protect from light

顏色

white

溶解度

water: 1 mg/mL

運輸包裝

ambient

儲存溫度

2-8°C

InChI

1S/C20H25ClN2O.ClH/c1-3-22(4-2)13-7-8-14-23-17-9-5-6-10-19(17)24-20-12-11-16(21)15-18(20)23;/h5-6,9-12,15H,3-4,7-8,13-14H2,1-2H3;1H

InChI 密鑰

SVKSJUIYYCQZEC-UHFFFAOYSA-N

一般說明

Akt磷酸化及其体外激酶活性(完全抑制<5 M) with minimal effect on PI 3-K, PDK1, or SGK1. Shown to suppress growth of Rh (rhabdomyosarcoma) cell lines (IC50 = 2-5 M), inhibit IGF-I-stimulated nuclear translocation of Akt, and prevent phosphorylation of the downstream targets, mTOR, p70S6 kinase, and S6 ribosomal protein. Unlike Akti1/2 (Cat. No. 124018), the mode of inhibition is not PH domain-dependent. Also shown to induce neuronal autophagy in an Akt- and mTOR-independent manner and enhances the clearance of misfolded protein. Also available as a 20 mM solution in H2O(Cat. No. 124039 )的细胞可渗透性、可逆性和选择性抑制剂。
Akt磷酸化及其体外激酶活性(完全抑制<5 µM)的细胞可渗透性、可逆性和选择性抑制剂,对PI 3-K、PDK1或SGK1的影响最小。显示可抑制Rh(横纹肌肉瘤)细胞系的生长(IC50 = 2-5 μM),抑制IGF-1刺激的Akt核易位,并防止下游靶标,mTOR,p70S6激酶和S6核糖体蛋白的磷酸化。与Akti1/2(目录编号124018)不同,抑制方式不是PH结构域依赖性的。还显示以Akt和mTOR独立的方式诱导神经元自噬,并增强错误折叠蛋白的清除率。

生化/生理作用

主靶
Akt
二级靶标
Rn细胞系(IC₅₀ = 2-5 µM)
产物不与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:<5 µM 抗Akt;2-5 µM 抗Rh(横纹肌肉瘤)细胞系生长

包裝

用惰性气体包装

警告

毒性:刺激性(B)

重構

在复溶后分装并冻存(-20°C)。储备溶液在-20°C下可稳定保存至多3个月。

其他說明

Tsvetkov, A.S., et al. 2010.Proc.Natl.Acad.Sci. USAin press.
Thimmaiah, K.N., et al. 2005.J. Biol. Chem.280, 31924.

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 1

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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