AKT Inhibitor IV

Name: AKT Inhibitor IV
Brand: Tocris Bioscience
SKU: 5985

Catalog # 5985

COA / SDS

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Key Product Details

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)
Molecular Weight:	614.54

View Full Technical Details for AKT Inhibitor IV

Biological Activity

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 50 = 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

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

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

Preparing Stock Solutions

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

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References

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

Meinig & Peterson Anticancer/antiviral agent Akt inhibitor-IV massively accumulates in mitochondria and potently disrupts cellular bioenergetics. ACS.Chem.Biol. 2015 PMID: 25415586
Sun Synthesis and biological evaluation of analogues of AKT (protein kinase B) inhibitor-IV. J.Med.Chem 2011 PMID: 21319800
Kau A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell. 2003 PMID: 14706338

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