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Submit ReviewAKT Inhibitor IV promotes hyperphosphorylation of Akt (Protein kinase B), decreases phosphorylation of Akt substrates, and inhibits FOXO1a nuclear export (IC50 = 625 nM in PTEN-null cells). AKT Inhibitor IV inhibits the proliferation of several cells lines (IC50 values are <1.25 μM, 320 - 670 nM and 340 nM for 786-O, HeLa and Jurkat cells, respectively). This compound also displays broad antiviral activity against negative-stranded RNA viruses; inhibits replication of parainfluenza virus 5 (PIV5) in HeLa cells (IC50 = 520 nM). In HeLa cells, AKT Inhibitor IV accumulates in mitochondria, disrupting morphology and increasing ROS production. At high concentrations (10 μM), AKT Inhibitor IV activates the unfolded protein response and apoptosis in HEK293T cells.
AKT Inhibitor IV is weakly fluorescent upon irradiation with UV light (excitation/emission maxima λ ~ 388/460; quantum yield = 0.0016).
M. Wt | 614.54 |
Formula | C31H27IN4S |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 959841-49-7 |
PubChem ID | 5719375 |
InChI Key | NAYRELMNTQSBIN-UHFFFAOYSA-M |
Smiles | CCN1C2=CC(C3=NC4=CC=CC=C4S3)=CC=C2[N+](C5=CC=CC=C5)=C1/C=C/N(C6=CC=CC=C6)C.[I-] |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 61.45 | 100 |
The following data is based on the product molecular weight 614.54. 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 |
---|---|---|---|
1 mM | 1.63 mL | 8.14 mL | 16.27 mL |
5 mM | 0.33 mL | 1.63 mL | 3.25 mL |
10 mM | 0.16 mL | 0.81 mL | 1.63 mL |
50 mM | 0.03 mL | 0.16 mL | 0.33 mL |
References are publications that support the biological activity of the product.
Kau et al (2003) A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell. 4 463 PMID: 14706338
Sun et al (2011) Synthesis and biological evaluation of analogues of AKT (protein kinase B) inhibitor-IV. J.Med.Chem 54 1126 PMID: 21319800
Meinig & Peterson (2015) Anticancer/antiviral agent Akt inhibitor-IV massively accumulates in mitochondria and potently disrupts cellular bioenergetics. ACS.Chem.Biol. 10 570 PMID: 25415586
If you know of a relevant reference for AKT Inhibitor IV, please let us know.
Keywords: AKT Inhibitor IV, AKT Inhibitor IV supplier, AKTIV, Akt, inhibitor, IV, Chembridge, 5233705, anticancer, antiviral, 681281-88-9, (Protein, Kinase, B), Non-selective, Antivirals, 5985, Tocris Bioscience
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