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API-2

Catalog #: 2151
17 Citations Datasheet / COA / SDS
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2151/10
API-2 | CAS No. 35943-35-2 | Akt (Protein Kinase B) Inhibitors
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Description: Selective inhibitor of Akt/PKB signaling. Antitumor and antiviral
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

Purity: ≥99%

Product Details
Citations (17)
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Biological Activity

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.

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

Background References

  1. AKT hyperactivation confers a Th1 phenotype in thymic Treg cells deficient in TGF-beta receptor II signaling.
    Liu Y, Xu Y, Sun J, Ma A, Zhang F, Xia S, Xu G, Liu Y
    Eur J Immunol, 2014;44(2):521-32.
  2. A personalized preclinical model to evaluate the metastatic potential of patient-derived colon cancer initiating cells.
    Puig I, Chicote I, Tenbaum S, Arques O, Herance J, Gispert J, Jimenez J, Landolfi S, Caci K, Allende H, Mendizabal L, Moreno D, Charco R, Espin E, Prat A, Elez M, Argiles G, Vivancos A, Tabernero J, Rojas S, Palmer H
    Clin Cancer Res, 2013;19(24):6787-801.
  3. Phenylbutyrate induces cathelicidin expression via the vitamin D receptor: Linkage to inflammatory and growth factor cytokines pathways.
    Kulkarni N, Yi Z, Huehnken C, Agerberth B, Gudmundsson G
    Mol Immunol, 2015;63(2):530-9.
  4. Tankyrase Inhibition Blocks Wnt/beta-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer.
    Arques O, Chicote I, Puig I, Tenbaum S, Argiles G, Dienstmann R, Fernandez N, Caratu G, Matito J, Silberschmidt D, Rodon J, Landolfi S, Prat A, Espin E, Charco R, Nuciforo P, Vivancos A, Shao W, Tabernero J, Palmer H
    Clin Cancer Res, 2016;22(3):644-56.
  5. beta-catenin confers resistance to PI3K and AKT inhibitors and subverts FOXO3a to promote metastasis in colon cancer.
    Tenbaum SP, Ordonez-Moran P, Puig I, Chicote I, Arques O, Landolfi S, Fernandez Y, Herance JR, Gispert JD, Mendizabal L, Aguilar S, Ramon y Cajal S, Schwartz S, Vivancos A, Espin E, Rojas S, Baselga J, Tabernero J, Munoz A, Palmer HG
    Nat. Med., 2012;18(6):892-901.
  6. Dual mechanisms of inhibition of DNA synthesis by triciribine.
    Wotring et al.
    Cancer Res., 1990;50:4891
  7. Phosphorylation of triciribine is necessary for activity against HIV type 1.
    Ptak et al.
    AIDS Res.Hum.Retroviruses., 1998;14:1315
  8. Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumour activity in cancer cells overexpressing Akt.
    Yang et al.
    Cancer Res., 2004;64:4394

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Citations for API-2

The citations listed below are publications that use Tocris products. Selected citations for API-2 include:

17 Citations: Showing 1 - 10

  1. IFT80 is required for stem cell proliferation, differentiation, and odontoblast polarization during tooth development.
    Authors: Yuan Et al.
    Cell Death Dis  2019;10:63
  2. The AKT inhibitor triciribine in combination with PTX has order-specific efficacy against Zfp217-induced breast cancer chemoresistance.
    Authors: Suarez Et al.
    Oncotarget  2017;8:108534
  3. Isolation and characterization of a new naturally immortalized human breast carcinoma cell line, KAIMRC1.
    Authors: Ali Et al.
    BMC Cancer  2017;17:803
  4. Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer.
    Authors: Arqu&eacutes Et al.
    Clin Cancer Res  2016;22:644
  5. Targeting Glutamatergic Signaling and the PI3 Kinase Pathway to Halt Melanoma Progression.
    Authors: Rosenberg Et al.
    Biol Open  2015;8:42614
  6. PI3K Phosphorylation Is Linked to Improved Electrical Excitability in an In Vitro Engineered Heart Tissue Disease Model System.
    Authors: Kana Et al.
    Tissue Eng Part A  2015;21:2379
  7. Repression of glucocorticoid-stimulated angiopoietin-like 4 gene transcription by Ins.
    Authors: Kuo Et al.
    J Lipid Res  2014;55:919
  8. PropF. mediates signal transducer and activator of transcription 3 activation and crosstalk with phosphoinositide 3-kinase/AKT.
    Authors: Shravah Et al.
    Am J Physiol Renal Physiol  2014;3:e29554
  9. Sea urchin akt activity is Runx-dependent and required for post-cleavage stage cell division.
    Authors: Robertson Et al.
    Blood  2013;2:472
  10. Calpain-mediated processing of p53-associated parkin-like cytoplasmic protein (PARC) affects chemosensitivity of human ovarian cancer cells by promoting p53 subcellular trafficking.
    Authors: Woo Et al.
    J Biol Chem  2012;287:3963

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