124020
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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所有图片(1)
About This Item
经验公式（希尔记法）:
C20H25ClN2O · xHCl
CAS号:
分子量:
344.88 (free base basis)
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
white
溶解性
water: 1 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
[Cl-].Clc1cc2c(cc1)Oc3c(cccc3)N2CCCC[N+H](CC)CC
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 key
SVKSJUIYYCQZEC-UHFFFAOYSA-N
一般描述
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
Akt
二级靶标
Rn细胞系（IC₅₀ = 2-5 µM）
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
包装
用惰性气体包装
警告
毒性：刺激性（B）
重悬
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。
其他说明
Tsvetkov, A.S., et al. 2010.Proc.Natl.Acad.Sci. USAin press.
Thimmaiah, K.N., et al. 2005.J. Biol. Chem.280, 31924.
Thimmaiah, K.N., et al. 2005.J. Biol. Chem.280, 31924.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Paola Di Pietro et al.
Antioxidants (Basel, Switzerland), 13(1) (2024-01-22)
High glucose-induced endothelial dysfunction is an important pathological feature of diabetic vasculopathy. While genome-wide studies have identified an association between type 2 diabetes mellitus (T2DM) and increased expression of a C2 calcium-dependent domain containing 4B (C2CD4B), no study has yet
Albino Carrizzo et al.
Antioxidants (Basel, Switzerland), 10(8) (2021-08-28)
In recent years, epidemiological studies have identified a relationship between diet and cerebro-cardiovascular disease (CVD). In this regard, there is a promising dietary group for cardiovascular protection are polyphenols, especially anthocyanins. Vascular reactivity studies were performed using Healthberry 865® and
Miji Jeon et al.
The Journal of biological chemistry, 298(3), 101675-101675 (2022-02-06)
A multienzyme metabolic assembly for human glucose metabolism, namely the glucosome, has been previously demonstrated to partition glucose flux between glycolysis and building block biosynthesis in an assembly size-dependent manner. Among three different sizes of glucosome assemblies, we have shown
Ryota Inoue et al.
iScience, 25(7), 104603-104603 (2022-07-09)
Uncoupling protein 2 (UCP2), a mitochondrial protein, is known to be upregulated in pancreatic islets of patients with type 2 diabetes (T2DM); however, the pathological significance of this increase in UCP2 expression is unclear. In this study, we highlight the
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