AKT Inhibitor IV

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Description: Promotes Akt hyperphosphorylation; decreases phosphorylation of Akt substrates
Chemical Name: 6-(2-Benzothiazolyl)-1-ethyl-2-[(1E)-2-(methylphenylamino)ethenyl]-3-phenyl-1H-benzimidazolium iodide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Pathways (1)

Biological Activity for AKT Inhibitor IV

AKT 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).

Technical Data for AKT Inhibitor IV

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.

Solubility Data for AKT Inhibitor IV

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 61.45 100

Preparing Stock Solutions for AKT Inhibitor IV

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for AKT Inhibitor IV

References for AKT Inhibitor IV

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


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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

Citations for AKT Inhibitor IV

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Pathways for AKT Inhibitor IV

Akt Signaling Pathway

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.