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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).
分子量 | 614.54 |
公式 | C31H27IN4S |
储存 | Store at -20°C |
纯度 | ≥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-] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 61.45 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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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