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Description: Potent and selective dual Akt1 and 2 inhibitor
Alternative Names: Akt Inhibitor VIII
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% (HPLC)
Citations (11)
Reviews (2)
Pathways (1)

Biological Activity for Akti-1/2

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 for Akti-1/2

M. Wt 551.64
Formula C34H29N7O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 612847-09-3
PubChem ID 10196499
Smiles O=C1NC2=C(C=CC=C2)N1C(CC3)CCN3CC(C=C4)=CC=C4C5=NC6=CC(N=CN7)=C7C=C6N=C5C8=CC=CC=C8

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.

Solubility Data for Akti-1/2

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 11.03 20 with gentle warming

Preparing Stock Solutions for Akti-1/2

The following data is based on the product molecular weight 551.64. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.06 mL 45.32 mL 90.64 mL
1 mM 1.81 mL 9.06 mL 18.13 mL
2 mM 0.91 mL 4.53 mL 9.06 mL
10 mM 0.18 mL 0.91 mL 1.81 mL

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Product Datasheets for Akti-1/2

Certificate of Analysis / Product Datasheet
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References for Akti-1/2

References are publications that support the biological activity of the product.

DeFeo-Jones D et al (2005) Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol.Cancer Ther. 4 271 PMID: 15713898

Barnett et al (2005) Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem. J. 385 399 PMID: 15456405

Lindsley et al (2005) Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg.Med.Chem.Lett. 15 761 PMID: 15664853

Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214

Klebanoff et al (2017) Inhibition of AKT signaling uncouples T cell differentiation from expansion for receptor-engineered adoptive immunotherapy. JCI Insight 2 e95103 PMID: 29212954

If you know of a relevant reference for Akti-1/2, please let us know.

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View all Akt (Protein Kinase B) Inhibitors

Keywords: Akti-1/2, Akti-1/2 supplier, Akt1/2, inhibitors, inhibits, potent, selective, PKB, protein, kinase, B, sensitizes, apoptosis, viral, transduction, enhancer, enhances, Akt, Inhibitor, VIII, (Protein, Kinase, B), Protein, B/Akt, Viral, Transduction, Enhancers, 5773, Tocris Bioscience

11 Citations for Akti-1/2

Citations are publications that use Tocris products. Selected citations for Akti-1/2 include:

Viviana I et al (2019) Wnt-induced activation of glucose metabolism mediates the in vivo neuroprotective roles of Wnt signaling in Alzheimer disease. J Neurochem 149 54-72 PMID: 30300917

Claudio et al (2022) PD-1-induced T cell exhaustion is controlled by a Drp1-dependent mechanism. Mol Oncol 16 188-205 PMID: 34535949

Aurélie et al (2022) Exosomes from EGFR-Mutated Adenocarcinoma Induce a Hybrid EMT and MMP9-Dependant Tumor Invasion. Cancers (Basel) 14 PMID: 35954442

Lucie et al (2022) Regulation of Stress-Activated Kinases in Response to Tacaribe Virus Infection and Its Implications for Viral Replication. Viruses 14 PMID: 36146824

Do you know of a great paper that uses Akti-1/2 from Tocris? Please let us know.

Reviews for Akti-1/2

Average Rating: 4.5 (Based on 2 Reviews.)

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Akti-1/2 blocks LPA-mediated COX-2 expression.
By Peter Cruz on 12/13/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma

Human osteosarcoma cells were incubated with 10 μM Akti-1/2 for 30 min prior to treatment with 10 μM LPA to estimate COX-2 expression using Western blot analysis. Akti-1/2 abolished LPA-induced COX-2 expression.

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Akt-1/2 blocks 15d-PGJ2-induced Akt phosphorylation.
By Christopher Trummer on 10/15/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: MG-63 osteosarcoma cells

MG-63 cells were incubated with PD169316 (25 μM), LY294002 (10 μM) or Akt-1/2 (5 μM Akt-I) for 30 min prior to 15d-PGJ2 treatment (20 μM) for 1 h to follow pAkt expression using Western blot. Akt-1/2 completely blocked 15d-PGJ2-induced Akt phosphorylation in MG-63 cells.

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Pathways for Akti-1/2

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.