Triciribine
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.
Triciribine是DNA合成的抑制剂，对Akt和HIV-1的IC50值分别为130 nM和20 nM[1,2]。
蛋白激酶B（PKB），亦称Akt，是一种丝氨酸/苏氨酸特异性蛋白激酶，在多种细胞进程中发挥重要作用，如葡萄糖代谢、细胞凋亡、细胞增殖、转录和细胞迁移。一旦Akt的PH域结合磷酸酯，活化的Akt可以通过其激酶活性继续激活或者去活化其多种底物，如核因子-κB、Bcl-2家族蛋白和鼠双微粒体2（MDM2）[3]。研究表明，具有持续活化Akt的肿瘤细胞依赖Akt而存活[4]。所以Akt抑制剂可能用于治疗肿瘤。
Triciribine也称为API-2，抑制Akt的磷酸化水平和激酶活性，诱导癌细胞凋亡，抑制细胞生长。Triciribine能特异性抑制大部分常见星形细胞瘤细胞，抑制效率非常低（GI50值为13.6 mM [5]）。Triciribine能抑制HIV-1，IC50值为20 nM。0.1 M的抑制率超过90%，5 M则会完全抑制多核细胞。HIV-1感染的CEM-SS、H9及p24核心抗原B和U1持续感染的H9III细胞中的毒性试验表明Triciribine浓度的选择范围为46 M至2250，Triciribine能以剂量依赖的方式显著抑制HIV-1诱导产生、逆转录酶以及感染病毒的产生[6]。Triciribine抑制人前列腺癌细胞系PC-3 Akt 308位酸和473位丝氨酸磷酸化和Akt活性。Triciribine能使PC-3细胞对TRAIL和anti-CD95诱导的凋亡更加敏感，但仍然耐受化疗引起的DNA损伤[7]。Triciribine也能选择性抑制Akt1、Akt2和Akt3，而不抑制已知的Akt上游激活剂PDK1和PI3K。此外，低微摩尔和亚微摩尔浓度的Triciribine具有抗肿瘤和抗病毒活性，其也能抑制氨基酸掺入蛋白质及嘌呤核苷酸合成。
参考文献：
1 Gursel DB, et al. “Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies”. Nero Oncol, 2011, 13(6), 610-621.
2 Kucera LS, et al, AIDS Res Hum Retroviruses, 1993, 9(4), 307-314.
3 Song G, Ouyang G, Bao S. "The activation of Akt/PKB signaling pathway and cell survival". J. Cell. Mol. Med, 2005, 9 (1): 59-71.
4 Lindhurst MJ, Sapp JC, Teer JK, Johnston JJ, Finn EM, Peters K et al. "A mosaic activating mutation in AKT1 associated with the Proteus syndrome". N. Engl. J. Med, 2011, 365 (7): 611-9.
5 Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621.
6 Dieterle A, et al, Int J Cancer , 2009, 125(4), 932-941.
7 Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399.
- 1. Jason J Northey, Alexander S Barrett, et al. "Stiff stroma increases breast cancer risk by inducing the oncogene ZNF217." J Clin Invest. 2020 Nov 2;130(11):5721-5737. PMID:32721948
- 2. Li Y, Yang Y, et al. "Astragaloside IV reduces neuronal apoptosis and parthanatos in ischemic injury by preserving mitochondrial hexokinase-II." Free Radic Biol Med. 2019 Feb 1;131:251-263. PMID:30502455
- 3. Du Q, Zhang S, et al. "Astragaloside IV Inhibits Adipose Lipolysis and Reduces Hepatic Glucose Production via Akt Dependent PDE3B Expression in HFD-Fed Mice." Front Physiol. 2018 Jan 23;9:15. PMID:29410630
- 4. Qun Liu, Fei-Ge Zhang, et al. "Ginsenoside Rg1 Inhibits Glucagon-Induced Hepatic Gluconeogenesis through Akt-FoxO1 Interaction."Theranostics 2017; 7(16):4001-4012.
- 5. Song J, Li Y, et al. "Mangiferin protects mitochondrial function by preserving mitochondrial hexokinase-II in vessel endothelial cells."Biochim Biophys Acta. 2017 Jul;1863(7):1829-1839. PMID:28478227
- 6. Yang YL, Li J, et al. "Ginsenoside Rg5 increases cardiomyocyte resistance to ischemic injury through regulation of mitochondrial hexokinase-II and dynamin-related protein 1." Cell Death Dis. 2017 Feb 23;8(2):e2625. PMID:28230856
| Storage | Store at -20°C |
| M.Wt | 320.3 |
| Cas No. | 35943-35-2 |
| Formula | C13H16N6O4 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥118.4 mg/mL in DMSO |
| Chemical Name | (2R,3R,4S,5R)-2-(3-amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol |
| SDF | Download SDF |
| Canonical SMILES | [H][C@](N1C(N=C([H])N=C2N(C([H])([H])[H])N=C3N([H])[H])=C2C3=C1[H])([C@]4([H])O[H])O[C@@](C([H])([H])O[H])([H])[C@@]4([H])O[H] |
| 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 [1-3]: | |
|
细胞系 |
星形细胞瘤细胞，HIV-1，PC-3细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度大于118.4mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
|
反应条件 |
IC50: 130 nM (Akt), IC50: 0.02-0.46 μM (HIV-1/2) |
|
应用 |
Triciribine（1-10 μM）抑制Nf1和Trp53突变型星形细胞瘤细胞中的细胞生长。Triciribine（100 μM）抑制Akt和p70S6K的磷酸化至基础水平。Triciribine不完全抑制WHO II K1861-10细胞系，GI50值为1.7 μM。在较低的GI50值（0.4-1.1 μM）下，Triciribine能够更大程度地抑制肿瘤细胞系（KR158、KR130和SF295）。Triciribine抑制HIV-1，IC50为20 nM。Triciribine（5 μM）完全抑制合胞体形成。在HIV-1急性感染的CEM-SS、H9和持续感染的H9IIIB和U1细胞中，Triciribine以剂量依赖性方式显著抑制HIV-1诱导的p24核心抗原产生、逆转录酶和感染性病毒产生。Triciribine抑制人前列腺癌细胞系PC-3中Akt蛋白Thr308和Ser473的磷酸化和Akt活性。 |
| 动物实验 [4]: | |
|
动物模型 |
携带OVCAR3、OVCAR8和PANC1肿瘤的裸鼠 |
|
给药剂量 |
腹腔注射，1 mg/kg/day，7 days |
|
应用 |
Triciribin抑制OVCAR3、OVCAR8和PANC1肿瘤生长。 |
|
注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
|
References: [1]. Gürsel D B, Connell-Albert Y S, Tuskan R G, et al. Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies[J]. Neuro-oncology, 2011, 13(6): 610-621. [2]. KUCERA L S, IYER N P, PUCKETT S H, et al. Activity of triciribine and triciribine-5′-monophosphate against human immunodeficiency virus types 1 and 2[J]. AIDS research and human retroviruses, 1993, 9(4): 307-314. [3]. Dieterle A, Orth R, Daubrawa M, et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL‐induced apoptosis[J]. International journal of cancer, 2009, 125(4): 932-941. [4]. Yang L, Dan H C, Sun M, et al. Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt[J]. Cancer research, 2004, 64(13): 4394-4399. |
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| Description | Triciribine是DNA合成的抑制剂，对Akt和HIV-1的IC50值分别为130 nM和20 nM。 | |||||
| 靶点 | HIV-1 | Akt | ||||
| IC50 | 20 nM | 130 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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