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BX517(PDK1 inhibitor2)PDK1 inhibitor

BX517(PDK1 inhibitor2)

Catalog No. B5838
Size Price Stock Qty
5mg $350.00 In stock
25mg $900.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BX517(PDK1 inhibitor2)

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Chemical Properties

Cas No. 850717-64-5 SDF Download SDF
Chemical Name (Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid
Canonical SMILES C/C(C1=CC=CN1)=C(C(O)=N2)\C3=C2C=CC(NC(O)=N)=C3
Formula C15H14N4O2 M.Wt 282.3
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.