Akti-1/2

Name: Akti-1/2
Brand: Tocris Bioscience
SKU: 5773
Rating: 5 (2 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 5773

Citations (3)

(2)

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Key Product Details

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)
Molecular Weight:	551.64

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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
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 for Akti-1/2

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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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References for Akti-1/2

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

Klebanoff Inhibition of AKT signaling uncouples T cell differentiation from expansion for receptor-engineered adoptive immunotherapy. JCI Insight 2017 PMID: 29212954
Bain The selectivity of protein kinase inhibitors: a further update. Biochem.J. 2007 PMID: 17850214
DeFeo-Jones D Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol.Cancer Ther. 2005 PMID: 15713898
Barnett Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem. J. 2005 PMID: 15456405
Lindsley Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg.Med.Chem.Lett. 2005 PMID: 15664853

Citations for Akti-1/2 (3)

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Citations are publications that use Bio-Techne 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
Perkins et al. (2018) Autocrine-paracrine prostaglandin E₂ signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol.. 19:1309
PMID: 30397349
Zhong et al. (2018) Tyro3 is a podocyte protective factor in glomerular disease. JCI Insight. 3
PMID: 30429374

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Customer Reviews for Akti-1/2 (2)

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Akti-1/2 blocks LPA-mediated COX-2 expression

Name: Peter Cruz

Species: Human

Assay Type: In Vitro

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.
Akt-1/2 blocks 15d-PGJ2-induced Akt phosphorylation

Name: Christopher Trummer

Species: Human

Assay Type: In Vitro

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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Product Documents for Akti-1/2

COA

Certificate of Analysis

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