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Submit ReviewAkti-1/2
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
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. Active in vivo.
Technical Data
| M. Wt | 551.64 |
| Formula | C34N29N7O |
| 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.
| 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
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
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, Akt, Inhibitor, VIII, (Protein, Kinase, B), Protein, B/Akt, 5773, Tocris Bioscience
2 Citations for Akti-1/2
Citations are publications that use Tocris products. Selected citations for Akti-1/2 include:
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.
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
