AG-CR1-3663-M0011 mgCHF 120.00
AG-CR1-3663-M0055 mgCHF 440.00
|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO (15mg/ml), ethanol (10mg/ml) or DMF (20mg/ml).|
|Identity||Determined by 1H-NMR.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
Keep cool and dry.
Keep under inert gas.
Protect from moisture and oxygen.
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent and selective Akt inhibitor (Ki=160pmol/L for all three isoforms PKBα, PKBβ and PKBγ).
- DYRK1A inhibitor (IC50=10nM). Inhibits other kinases, including PRK2, MSK1 and DYRK3 at low nM range as well.
- Interferes with mitotic progression by regulating aurora a kinase expression and bipolar spindle formation. It induces G2/M accumulation, defects in centrosome separation and formation of either monopolar arrays or disorganized spindles.
- Anticancer agent. Apoptosis inducer and chemosensitizing agent. Slows the progression and growth of Akt-dependent tumors.
- Induces rapid Akt Ser473 phosphorylation independent of mTORC1 inhibition in human cancer cell lines.
- Activates mTORC2 and reverses long-term memory deficits.
- Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo: L. Luo, et al.; Mol. Cancer Ther. 4, 977 (2005)
- Akt inhibitor A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition: E.K. Han, et al.; Oncogene 26, 5655 (2007)
- A role for Akt in epidermal growth factor-stimulated cell cycle progression in cultured hepatocytes: generation of a hyperproliferative window after adenoviral expression of constitutively active Akt: Y. Luo, et al.; J. Pharmacol. Exp. Ther. 321, 884 (2007)
- The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007)
- Proapoptotic activity and chemosensitizing effect of the novel Akt inhibitor (2S)-1-(1H-Indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan2-amine (A443654) in T-cell acute lymphoblastic leukemia: F. Fala, et al.; Mol. Pharmacol. 74, 884 (2008)
- Akt inhibitor a-443654 interferes with mitotic progression by regulating aurora a kinase expression: X. Liu, et al.; Neoplasia 10, 828 (2008)
- Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells: G.L. Gallia, et al.; Mol. Cancer Ther. 8, 386 (2009)
- Akt inhibitors induce apoptosis in chronic lymphocytic leukemia cells: M. de Frias, et al.; Haematologica 94, 1698 (2009)
- An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo: C. Cherrin, et al.; Cancer Biol. Ther. 9, 493 (2010)
- Recent Advances in the Design, Synthesis, and Biological Evaluation of Selective DYRK1A Inhibitors: A New Avenue for a Disease Modifying Treatment of Alzheimer's: B. Smith, et al.; ACS Chem. Neurosci. 3, 857 (2012)
- TORC2: a novel target for treating age-associated memory impairment: J.L. Johnson, et al.; Sci. Rep. 5, 15193 (2015)