Biological Activity
Inhibitor of 3-phosphoinositide-dependent kinase 1 (PDPK1). Inhibits Akt phosphorylation at Thr308 in PC3 cells; also inhibits anchorage-independent growth of PC3 and MDA-MB-468 cells. Exhibits activity at other kinases, including TANK-binding kinase 1 (TBK1), Aurora B and IκB kinase ε (IKKε).
Technical Data
| M. Wt | 591.47 |
| Formula | C23H26IN7O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 702675-74-9 |
| PubChem ID | 10077147 |
| InChI Key | VAVXGGRQQJZYBL-UHFFFAOYSA-N |
| Smiles | IC1=C(NCCCNC(C4=CC=CS4)=O)N=C(NC2=CC(NC(N3CCCC3)=O)=CC=C2)N=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 59.15 | 100 | |
| ethanol | 59.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 591.47. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 1.69 mL | 8.45 mL | 16.91 mL |
| 5 mM | 0.34 mL | 1.69 mL | 3.38 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.69 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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References
References are publications that support the products' biological activity.
Feldman et al (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J.Biol.Chem. 280 19867 PMID: 15772071
Clark et al (2009) Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IκB kinase ε: a distinct upstream kinase mediates Ser-172 phosphorylation and activati J.Biol.Chem. 284 14136 PMID: 19307177
Tamguney et al (2008) Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp.Cell Res. 314 2299 PMID: 18514190
Keywords: BX 795, supplier, BX795, pdk1, inhibitors, inhibits, 3-phosphoinositide-dependent, kinase-1, TBK1, TANK-binding, kinase, 1, Aurora, B, IkBe, IkappaBepsilon, IκBε, kinase, multi-kinase, PDPK1, Phosphoinositide-dependent, Kinase, 1, PDK1, Phosphoinositide-dependent, Kinase, 1, Tocris Bioscience
