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.

Product information

CAS Number: 959841-49-7

Molecular Weight: 614.54

Formula: C31H27IN4S

Chemical Name: 6-(2-Benzothiazolyl)-1-ethyl-2-[(1E)-2-(methylphenylamino)ethenyl]-3-phenyl-1H-benzimidazolium iodide

Smiles: [I-].CN(/C=C/C1N(CC)C2=CC(=CC=C2[N+]=1C1C=CC=CC=1)C1=NC2=CC=CC=C2S1)C1C=CC=CC=1

InChiKey: NAYRELMNTQSBIN-UHFFFAOYSA-M

InChi: InChI=1S/C31H27N4S.HI/c1-3-34-28-22-23(31-32-26-16-10-11-17-29(26)36-31)18-19-27(28)35(25-14-8-5-9-15-25)30(34)20-21-33(2)24-12-6-4-7-13-24;/h4-22H,3H2,1-2H3;1H/q+1;/p-1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. 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
2. Sun et al (2011) Synthesis and biological evaluation of analogues of AKT (protein kinase B) inhibitor-IV. J.Med.Chem 54 1126 PMID: 21319800
3. 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

Products are for research use only. Not for human use.