AKT inhibitor VIII
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AKT inhibitor VIII是一种细胞通透性的、可逆性的、有效的和选择性的Akt1、Akt2和Akt3抑制剂,IC550值分别为58 nM、210 nM和2119 nM。
在人类乳腺癌细胞MCF-7中,AKT inhibitor VIII可以显著增加furanodiene的抗增殖能力。AKT inhibitor VIII可以增强furanodiene引起的Akt和p-Akt表达的下调,并增加furanodiene诱发的PARP裂解[1]。
AKT inhibitor VIII以浓度依赖的方式抑制IGF-1诱导的Akt磷酸化。在PC12细胞中,AKT inhibitor VIII也可以减少PRAS40的磷酸化[2]。
参考文献:
[1] Zhong Z1, Dang Y, Yuan X, Guo W, Li Y, Tan W, Cui J, Lu J, Zhang Q, Chen X, Wang Y. Furanodiene, a natural product, inhibits breast cancer growth both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90.
[2] Wang H1, Zhang Q, Zhang L, Little PJ, Xie X, Meng Q, Ren Y, Zhou L, Gao G, Quirion R, Zheng W. Insulin-like growth factor-1 induces the phosphorylation of PRAS40 via the PI3K/Akt signaling pathway in PC12 cells. Neurosci Lett. 2012 May 10;516(1):105-9.
- 1. Yingwei Xie, Zhiliang Chen, et al. "M2 Macrophages Secrete CXCL13 to Promote Renal Cell Carcinoma Migration, Invasion, and EMT." Cancer Cell Int. 2021 Dec 18;21(1):677. PMID:34922542
- 2. Xiaowen Chen, Wenting Liu, et al. "FOXO3a accumulation and activation accelerate oxidative stress‐induced podocyte injury." FASEB J. 12 August 2020. PMID:32786113
- 3. Eldad TZAHOR,Gabriele Matteo D'UVA,et al. "Methods, kits and devices for promoting cardiac regeneration." US Patent App. 15, 2016.
- 4. D’Uva, Gabriele, et al. "ERBB2 triggers mammalian heart regeneration by promoting cardiomyocyte dedifferentiation and proliferation." Nature Cell Biology (2015). PMID:25848746
Storage | Store at -20°C |
M.Wt | 551.64 |
Cas No. | 612847-09-3 |
Formula | C34H29N7O |
Solubility | insoluble in H2O; insoluble in EtOH; ≥9.2 mg/mL in DMSO |
Chemical Name | 3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one |
SDF | Download SDF |
Canonical SMILES | C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=NC6=CC7=C(C=C6N=C5C8=CC=CC=C8)N=CN7 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
人类乳腺癌细胞(MCF-7) |
溶解方法 |
在DMSO中的溶解度> 9.2 mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
10-100μM;孵育24,48和72小时 |
应用 |
AKT inhibitor VIII是一种细胞通透性的、可逆性的、有效的和选择性的Akt1、Akt2和Akt3抑制剂。在人类乳腺癌细胞MCF-7中,AKT inhibitor VIII可以显著增加furanodiene的抗增殖能力。AKT inhibitor VIII可以增强furanodiene引起的Akt和p-Akt表达的下调,并增加furanodiene诱发的PARP裂解。 |
动物实验 [1]: | |
动物模型 |
MCF-7 Balb/c裸鼠荷瘤模型 |
剂量 |
15和30毫克/公斤,腹腔注射,一天一次连续给药8天 |
应用 |
AKT inhibitor VIII能够剂量依赖性地抑制裸鼠体内的肿瘤生长,在15和30毫克/公斤腹腔给药剂量下可以分别带来32% 以及54%的肿瘤体积的缩小。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Zhong Z, Dang Y, Yuan X, Guo W, Li Y, Tan W, Cui J, Lu J, Zhang Q, Chen X, Wang Y. Furanodiene, a natural product, inhibits breast cancer growth both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. |
描述 | AKT inhibitor VIII是一种有效的和选择性的Akt激酶变构抑制剂,对于Akt1、Akt2和Akt3的IC550值分别为58 nM、210 nM和2119 nM。 | |||||
靶点 | Akt1 | Akt2 | Akt3 | |||
IC50 | 58 nM | 210 nM | 2119 nM |
质量控制和MSDS
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