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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)
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 Data for Akti-1/2
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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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Product Datasheets for Akti-1/2
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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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:
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
Anna M et al (2021) Gαq activation modulates autophagy by promoting mTORC1 signaling. Nat Commun 12 4540 PMID: 34315875
Charles G et al (2021) EGFR Activates a TAZ-Driven Oncogenic Program in Glioblastoma. Cancer Res 81 3580-3592 PMID: 33910930
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
Adriano et al (2022) TSC22D4 interacts with Akt1 to regulate glucose metabolism. Sci Adv 8 eabo5555 PMID: 36269831
Margitta et al (2022) Pannexin-1 Activation by Phosphorylation Is Crucial for Platelet Aggregation and Thrombus Formation. Int J Mol Sci 23 PMID: 35563450
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.
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.
Pathways for Akti-1/2
