AKT-IN-6
目录号 : GC62190
AKT-IN-6是一种强效的泛AKT(Akt1/2/3)小分子抑制剂,体外对三种AKT亚型的IC50均小于500nM。
Cas No.:1430056-54-4
Sample solution is provided at 25 µL, 10mM.
AKT-IN-6 is a potent pan‑AKT (Akt1/2/3) small molecule inhibitor with an in vitro IC50 of less than 500nM for all three AKT isoforms [1]. AKT-IN-6 is primarily used to study the regulation of AKT activity in the PI3K/Akt/mTOR signaling pathway and its role in disease models such as cancer and metabolic diseases [2-3].
In tilapia S. agalactiae infection model, Treatment with AKT-IN-6 (1mg/kg; ip; 2d) significantly reduced the expression and phosphorylation levels of IKKα/β, IκBα, and NF-κB p65 [4].
References:
[1]. Huang T, Feng H, Kong L, et al. Isoindolinone and pyrrolopyridinone derivatives as Akt inhibitors. United States patent US 8,895,571. 2014 Nov 25.
[2]. Manning BD, Cantley LC. AKT/PKB signaling: navigating downstream. Cell. 2007 Jun 29; 129(7): 1261-1274.
[3]. Castro D, Castaner R, Fernandez-Forner D. NME Digest-January 2016. Drugs of the Future. 2016; 41(1).
[4]. Mu L, Li J, Lin Z, et al. MBL regulates phagocytosis and bactericidal activity of macrophages by triggering AKT/NF-κB/Rab5A axis occurred early in vertebrate evolution. The Journal of Immunology. 2025 Apr 25: vkaf028.
AKT-IN-6是一种强效的泛AKT(Akt1/2/3)小分子抑制剂,体外对三种AKT亚型的IC50均小于500nM [1]。AKT-IN-6主要用于研究PI3K/Akt/mTOR信号通路中AKT活性的调控及其在癌症和代谢性疾病等疾病模型中的作用 [2-3]。
在罗非鱼的S. agalactiae感染模型中,AKT-IN-6(1mg/kg;op;2d)治疗显著降低了IKKα/β、IκBα和NF-κB p65的表达和磷酸化水平 [4]。
Animal experiment [1]: | |
Animal models | Tilapia S. agalactiae infection model |
Preparation Method | Tilapia were intraperito neally injected with 1mg/kg AKT-IN-6 or IKK-16 during S. agalactiae (1×107CFU/mL) infection before the separation of head kidney MA. MA from inhibitor-treated or untreated tilapia were challenged with OnMBL for 12h, and the phosphorylation levels of indicated molecules were detected by Western blot. In addition, the phagocytic ability and ROS release levels of MA in the AKT-IN-6 treatment group were analyzed by flow cytometry. For the survival assay, tilapia were intraperitoneally injected with 1mg/kg AKT-IN-6 for 2 consecutive days. During this time, fish were also infected with 100μL of S. agalactiae (1×108CFU/mL) in the absence or presence of OnMBL at 24h after the first inhibitor injection. The daily deaths of tilapia were recorded. |
Dosage form | 1mg/kg; ip; 2d |
Applications | Treatment with AKT-IN-6 significantly reduced the expression and phosphorylation levels of IKKα/β, IκBα, and NF-κB p65. |
References: |
Cas No. | 1430056-54-4 | SDF | |
分子式 | C22H20FN5O | 分子量 | 389.43 |
溶解度 | DMSO : 125 mg/mL (320.98 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 2.5679 mL | 12.8393 mL | 25.6786 mL |
5 mM | 0.5136 mL | 2.5679 mL | 5.1357 mL |
10 mM | 0.2568 mL | 1.2839 mL | 2.5679 mL |
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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