API-2

Cat. No. 2151

API-2 C13H16N6O4 [35943-35-2]

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Alternative Names: Triciribine, NSC 154020, TCN

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

Biological Activity

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.

Technical Data

M.Wt:
320.31
Formula:
C13H16N6O4
Solubility:
Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at RT
CAS No:
35943-35-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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

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

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for API-2 include:

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

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

Shravah et al (2014) Propofol 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.

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.

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

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.

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.

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

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.

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Keywords: API-2, supplier, Selective, inhibitors, inhibits, Akt, PKB, signaling, Antitumor, antiviral, Protein, Kinase, B, NSC154020, Tocris Bioscience, Akt (Protein Kinase B) Inhibitor products

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