API-2

Cat. No. 2151 17 篇引用文献 1 条评论提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Selective inhibitor of Akt/PKB signaling. Antitumor and antiviral

别名： Triciribine,NSC 154020,TCN

化学名： 1,5-Dihydro-5-methyl-1-β-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine

纯度： ≥99% (HPLC)

说明书

引用文献 (17)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for API-2

API-2 is a selective inhibitor of Akt (protein kinase B) signaling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways. Inhibits phosphorylation and activation of downstream targets of Akt including Bad, GSK-3β and AFX. Induces apoptosis and growth arrest in vitro, preferentially in human cancer cells with elevated levels of Akt. Potently and selectively inhibits growth of Akt-overexpressing tumors in mice. Inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2.

化合物库 for API-2

API-2 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。

技术数据 for API-2

分子量	320.31
公式	C₁₃H₁₆N₆O₄
储存	Store at RT
纯度	≥99% (HPLC)
CAS Number	35943-35-2
PubChem ID	65399
InChI Key	HOGVTUZUJGHKPL-HTVVRFAVSA-N
Smiles	O[C@@H]1[C@@H](CO)O[C@@H](N2C3=C(C4=NC=N3)C(C(N)=NN4C)=C2)[C@@H]1O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for API-2

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	1eq. HCl	32.03	100
	DMSO	32.03	100

制备储备液 for API-2

以下数据基于产品分子量 320.31。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	3.12 mL	15.61 mL	31.22 mL
5 mM	0.62 mL	3.12 mL	6.24 mL
10 mM	0.31 mL	1.56 mL	3.12 mL
50 mM	0.06 mL	0.31 mL	0.62 mL

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产品说明书 for API-2

分析证书/产品说明书

化学品安全技术说明书

参考文献 for API-2

参考文献是支持产品生物活性的出版物。

Wotring et al (1990) Dual mechanisms of inhibition of DNA synthesis by triciribine. Cancer Res. 50 4891 PMID: 2379153

Ptak et al (1998) Phosphorylation of triciribine is necessary for activity against HIV type 1. AIDS Res.Hum.Retroviruses. 14 1315 PMID: 9788672

Yang et al (2004) Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumour activity in cancer cells overexpressing Akt. Cancer Res. 64 4394 PMID: 15231645

If you know of a relevant reference for API-2, please let us know.

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查看全部 Akt (Protein Kinase B) Inhibitors

关键词: API-2, API-2 supplier, Selective, inhibitors, inhibits, Akt, PKB, signaling, Antitumor, antiviral, Protein, Kinase, B, NSC154020, Triciribine, NSC, 154020, TCN, (Protein, B), B/Akt, HIV, 2151, Tocris Bioscience

17 篇 API-2 的引用文献

引用文献是使用了 Tocris 产品的出版物。 API-2 的部分引用包括：

Shravah et al (2014) PropF. mediates signal transducer and activator of transcription 3 activation and crosstalk with phosphoinositide 3-kinase/AKT. Am J Physiol Renal Physiol 3 e29554 PMID: 25105067

Robertson et al (2013) Sea urchin akt activity is Runx-dependent and required for post-cleavage stage cell division. Blood 2 472 PMID: 23789095

Yuan et al (2019) IFT80 is required for stem cell proliferation, differentiation, and odontoblast polarization during tooth development. Cell Death Dis 10 63 PMID: 30683845

Barber and Sentman (2011) NKG2D receptor regulates human effector T-cell cytokine production. Mol Cell 117 6571 PMID: 21518928

Kana et al (2015) PI3K Phosphorylation Is Linked to Improved Electrical Excitability in an In Vitro Engineered Heart Tissue Disease Model System. Tissue Eng Part A 21 2379 PMID: 26120935

Roselli et al (2009) Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways. PLoS One 4 e6011 PMID: 19547699

Arqués et al (2016) Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer. Clin Cancer Res 22 644 PMID: 26224873

Woo et al (2012) Calpain-mediated processing of p53-associated parkin-like cytoplasmic protein (PARC) affects chemosensitivity of human ovarian cancer cells by promoting p53 subcellular trafficking. J Biol Chem 287 3963 PMID: 22117079

Sunters et al (2010) Mechano-transduction in osteoblastic cells involves strain-regulated estrogen receptor alpha-mediated control of Ins-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 receptor-i J Biol Chem 285 8743 PMID: 20042609

Jackson et al (2010) Control of cerebellar long-term potentiation by P-Rex-family guanine-nucleotide exchange factors and phosphoinositide 3-kinase. PLoS One 5 e11962 PMID: 20694145

Liu et al (2010) FRP inhibits ox-LDL-induced endothelial cell apoptosis through an Akt-NF-{kappa}B-Bcl-2 pathway and inhibits endothelial cell apoptosis in an apoE-knockout mouse model. Am J Physiol Endocrinol Metab 299 E351 PMID: 20530739

Rosenberg et al (2015) Targeting Glutamatergic Signaling and the PI3 Kinase Pathway to Halt Melanoma Progression. Biol Open 8 42614 PMID: 25749171

Suarez et al (2017) The AKT inhibitor triciribine in combination with PTX has order-specific efficacy against Zfp217-induced breast cancer chemoresistance. Oncotarget 8 108534 PMID: 29312549

Ali et al (2017) Isolation and characterization of a new naturally immortalized human breast carcinoma cell line, KAIMRC1. BMC Cancer 17 803 PMID: 29187162

Kuo et al (2014) Repression of glucocorticoid-stimulated angiopoietin-like 4 gene transcription by Ins. J Lipid Res 55 919 PMID: 24565756

Duan et al (2011) mTOR generates an auto-amplification loop by triggering the βTrCP- and CK1α-dependent degradation of DEPTOR. JAKSTAT 44 317 PMID: 22017877

Madhunapantula et al (2007) PRAS40 deregulates apoptosis in malignant melanoma. Cancer Res 67 3626 PMID: 17440074

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Attenuation by co-treatment of either PI3K inhibitor LY94002 or Akt inhibitor API-2.

By Zhenmin Lei on 01/04/2018

分析类型： In Vitro

种属： Mouse

细胞系/组织： Ovarian theca cells

The isolated mouse ovarian theca cells were maintained in 12-well plates withRPMI-1640 medium. For determination of Lhcgr expression, thecells were rinsed three times with PBS the day before incubation with vehicle(DMSO), 740YP (50 mg/ml), 740YP + API-2 (7.5 mM), LH (50 ng/mL),or LH + API-2 for 24 h. For determination of Akt phosphorylation,PBS rinsed cells were incubated with vehicle (DMSO), or API-2 (7.5 mM) in serum-free RPMI-medium for 1 h before the addition of LH (50 ng/mL) for 30 min.

Pathways for API-2

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.