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ProductsBack/A-443654 [552325-16-3]
Chemical Structure
Chemical Structure
Chemical Structure

A-443654 [552325-16-3]

Research Use Only
AG-CR1-3663
AdipoGen Life Sciences
CAS Number552325-16-3
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight397.5
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    A-443654 [552325-16-3]
  • Delivery Days Customer
    10
  • CAS Number
    552325-16-3
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C24H23N5O
  • Molecular Weight
    397.5
  • Scientific Description
    Chemical. CAS: 552325-16-3. Formula: C24H23N5O. MW: 397.5. Synthetic. Potent and selective Akt inhibitor (Ki=160pmol/L for all three isoforms PKBalpha, PKBbeta and PKBgamma). 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 Akt inhibitor (Ki=160pmol/L for all three isoforms PKBalpha, PKBbeta and PKBgamma). 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.
  • SMILES
    N[C@@H](CC1=CNC2=C1C=CC=C2)COC3=CC(C4=CC(C(C)=NN5)=C5C=C4)=CN=C3
  • Storage Instruction
    2°C to 8°C,-20°C
  • UNSPSC
    12352200

References

  • 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)