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| | PDK1 Inhibitor Basic information |
| Product Name: | PDK1 Inhibitor | | Synonyms: | BX-517;BX517(PDK1 inhibitor2);5-Ureido-3-[1-(pyrrol-2-yl)ethylidene]indolin-2-one;PDK1 Inhibitor 2;CS-1693;PDK1 Inhibitor II;BX-517;BX 517;Urea, [2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]- | | CAS: | 850717-64-5 | | MF: | C15H14N4O2 | | MW: | 282.3 | | EINECS: | | | Product Categories: | | | Mol File: | 850717-64-5.mol |  |
| | PDK1 Inhibitor Chemical Properties |
| storage temp. | Store at -20°C | | solubility | insoluble in H2O; insoluble in EtOH; ≥8.55 mg/mL in DMSO | | form | solid |
| | PDK1 Inhibitor Usage And Synthesis |
| Uses | BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM). | | Biological Activity | bx-517 is a potent and selective inhibitor of pdk1 that binds to the atp binding pocketof the protein (ic50 = 6 nm). bx-517 also blocks activation of akt in tumor cells with 10-fold more potent (ic50 = 0.1–1.0 μm) than its analogs tested at the highest dose tested (10 μm). [1] the phosphoinositide-dependent kinase-1 (pdk1) is a ser/thr kinase that is a crucial activator of a range of protein kinases in the agc kinase super-family that play key roles in the progression of cancer and for the activation of akt, s6 kinase, and protein kinase c. [2] | | references | 1. islam i, brown g, bryant j et al. indolinone based phosphoinositide-dependentkinase-1 (pdk1) inhibitors. part 2: optimization of bx-517. bioorg med chem lett.2007 jul 15;17(14):3819-25. 2. islam i, bryant j, chou yl etc. indolinone based phosphoinositide-dependent kinase-1 (pdk1)inhibitors. part 1: design, synthesis and biological activity. bioorg med chem lett. 2007 jul 15;17(14):3814-8. |
| | PDK1 Inhibitor Preparation Products And Raw materials |
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