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BX517(PDK1 inhibitor2)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BX517(PDK1 inhibitor2)图片
CAS NO:850717-64-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)询价
5mg询价
10mg询价
25mg询价
50mg询价
100mg询价

BX517(PDK1 inhibitor2) 是一种有效的选择性 PDK1 抑制剂，IC50 为 6 nM。
Cas No.850717-64-5
化学名(Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid
Canonical SMILESC/C(C1=CC=CN1)=C(C(O)=N2)\C3=C2C=CC(NC(O)=N)=C3
分子式C15H14N4O2
分子量282.3
溶解度≥ 8.55mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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