Akti-1/2
Chemical Name: 1,3-Dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-2H-benzimidazol-2-one
Purity: ≥98%
Biological Activity
Akti-1/2 is a potent and selective dual Akt1 and 2 inhibitor (IC50 values are 50 and 210 nM, respectively). Selective for Akt1 and 2 over a panel of other tyrosine and serine/threonine kinases. Sensitizes LnCaP cells to TRAIL (TNF-related apoptosis-inducing ligand) induced apoptosis. Also enhances CAR and TCR retroviral transduction of human T cells. Active in vivo.Technical Data
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.
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Background References
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The selectivity of protein kinase inhibitors: a further update.
Bain et al.
Biochem.J., 2007;408:297 -
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members.
DeFeo-Jones D et al.
Mol.Cancer Ther., 2005;4:271 -
Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors.
Barnett et al.
Biochem. J., 2005;385:399 -
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Lindsley et al.
Bioorg.Med.Chem.Lett., 2005;15:761 -
Inhibition of AKT signaling uncouples T cell differentiation from expansion for receptor-engineered adoptive immunotherapy.
Klebanoff et al.
JCI Insight, 2017;2:e95103
Product Datasheets
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Citations for Akti-1/2
The citations listed below are publications that use Tocris products. Selected citations for Akti-1/2 include:
3 Citations: Showing 1 - 3
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Characterization of a novel compound that promotes myogenesis via Akt and transcriptional co-activator with PDZ-binding motif (TAZ) in mouse C2C12 cells.
Authors: Kodaka Et al.
PLoS One 2020;15:e0231265
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Tyro3 is a podocyte protective factor in glomerular disease.
Authors: Zhong Et al.
JCI Insight 2018;3
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Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling.
Authors: Perkins Et al.
Nat.Immunol. 2018;19:1309
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