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Dual Akt and PDK1 inhibitor; binds the pleckstrin homology (PH) domain of Akt and PDK1 (Ki values are 2.7 and 5.2 μM, respectively). Inhibits Akt phosphorylation and Akt downstream targets; also induces apoptosis in vitro. Displays synergistic antitumor effect when combined with chemotherapeutics in breast cancer mouse models.
|Storage||Store at -20°C|
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|
Preparing Stock Solutions
The following data is based on the product molecular weight 409.61. 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||2.44 mL||12.21 mL||24.41 mL|
|5 mM||0.49 mL||2.44 mL||4.88 mL|
|10 mM||0.24 mL||1.22 mL||2.44 mL|
|50 mM||0.05 mL||0.24 mL||0.49 mL|
References are publications that support the biological activity of the product.
Moses et al (2009) In vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase B/AKT. Cancer Res. 69 5073 PMID: 19491272
Meuillet et al (2010) Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol.Cancer Ther. 9 706 PMID: 20197390
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Keywords: PHT 427, PHT 427 supplier, PHT427, Phosphatidylinositol, 3-kinase/phosphatidylinositide-dependent, protein, kinase, 1, PDPK1Akt,, pleckstrin, homology, PH, domain, AKT, inhibitors, inhibits, antitumor, duel, tumour, PDK1, Akt, (Protein, Kinase, B), Protein, B/Akt, Phosphoinositide-dependent, 4598, Tocris Bioscience
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Literature in this Area
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.