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Akti-1/2

Cat. No. 5773 3 Citations 2 Reviews Submit a Review Datasheet / COA / SDS
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Cat.No. 5773 - Akti-1/2 | C34H29N7O | CAS No. 612847-09-3
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)
Datasheet
Citations (3)
Reviews (2)
Literature (3)
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

M. Wt 551.64
Formula C34H29N7O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 612847-09-3
PubChem ID 10196499
InChI Key BIWGYFZAEWGBAL-UHFFFAOYSA-N
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

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

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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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3 Citations for Akti-1/2

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

Kodaka et al (2020) Characterization of a novel compound that promotes myogenesis via Akt and transcriptional co-activator with PDZ-binding motif (TAZ) in mouse C2C12 cells. PLoS One 15 e0231265 PMID: 32267872

Zhong et al (2018) Tyro3 is a podocyte protective factor in glomerular disease. JCI Insight 3 PMID: 30429374

Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349

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.

review image
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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Literature in this Area

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Pathways for Akti-1/2

Akt

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.