BX517(PDK1 inhibitor2)
BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket
of 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-dependent
kinase-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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 282.3 |
| Cas No. | 850717-64-5 |
| Formula | C15H14N4O2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥8.55 mg/mL in DMSO |
| Chemical Name | (Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid |
| SDF | Download SDF |
| Canonical SMILES | C/C(C1=CC=CN1)=C(C(O)=N2)\C3=C2C=CC(NC(O)=N)=C3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
