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A6730 Sigma

Akt1/2 kinase inhibitor

≥98% (HPLC)

Synonym: 1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one trifluoroacetate salt hydrate, Akt Inhibitor VIII trifluoroacetate salt hydrate, Akti-1/2 trifluoroacetate salt hydrate

  • Empirical Formula (Hill Notation) C34H29N7O · xC2HF3O2 · yH2O

  • Molecular Weight 551.64 (anhydrous free base basis)

  •  MDL number MFCD08705407

  •  PubChem Substance ID 24891133

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Description

Application

Akt plays a role in signal transduction pathways of cell proliferation, apoptosis, angiogenesis, and diabetes. Akt1 and Akt2 dual kinase inhibitors are capable of sensitizing tumor cells to certain apoptotic stimuli, and inhibit Akt phosphorylation in vivo. Akt1 kinase activity and its regulation by extracellular signaling factors in vivo in hematopoietic cells suggests the activation of AKT1 involves intracellular translocation of the kinase from cytosol to membrane.

Biochem/physiol Actions

Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by Merck. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Price and Availability


DISCOVER Bioactive Small Molecules

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Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis

Protocols & Articles

Articles

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Phosphorylation is a ubiquitous cellular regulatory mechanism that mediates signal transduction pathways, which carry signals from the cell surface to the nucleus or cytoplasm, by altering the activi...
Keywords: Apoptosis, Bioactive small molecules, Cancer, Diseases, Inflammation, Metabolism, Neurodegenerative Diseases, Phosphorylations, Transduction

Oncogenes and Tumor Suppressors Reprogram Metabolism

Proliferating cells require the biosynthesis of structural components for biomass production and for genomic replication. This requires a reprogramming of the metabolic pathways to ensure nutrients s...
Keywords: Aerobic, Antitumor agents, Apoptosis, Biofiles, Cancer, Citric Acid Cycle, Degradations, Environmental, Events, Gene expression, Glycolysis, Growth factors, Metabolic Pathways, Metabolism, Metabolites, Nucleotide Synthesis, PAGE, Pentose phosphate pathway, Phosphorylations, Support

PKB/Akt

The PDK1–PKB/Akt axis represents one of the most actively researched cell signaling pathways. This protein kinase cascade is known to play a central role in mediating the actions of a range of stimul...
Keywords: Apoptosis, Atomic absorption spectroscopy, Cancer, Cell proliferation, Cell signaling, Diabetes, Gene expression, Growth factors, Inflammation, Metabolism, Myristoylations, Phosphorylations, Reversible addition-fragmentation chain transfer polymerizations

Peer-Reviewed Papers
15

References

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