GSK2334470

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	同义名 :	-
	CAS号 :	1227911-45-6
	货号 :	A202355
	分子式 :	C₂₅H₃₄N₈O
	纯度 :	99%+
	分子量 :	462.591
	MDL号 :	MFCD21608525
	存储条件：	Pure form Keep in dark place,Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	DMSO: 50 mg/mL(108.09 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
	动物实验配方：

生物活性
靶点	PDK1 PDK-1, IC50:10 nM
描述	PDK1 (3-phosphoinositide-dependent protein kinase 1) plays an important role in growth factor signalling cascades by phosphorylating and activating a group of protein kinases belonging to the AGC [PKA (protein kinase A)/PKG (proteinkinase G)/PKC (protein kinase C)]-kinase family. GSK2334470 inhibits PDK1 with an IC_₅₀ of ~10 nM. Addition of GSK2334470 to HEK (human embryonic kidney)-293, U87 or MEF (mouse embryonic fibroblast) cells ablated T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF1 (insulin-like growth factor 1). GSK2334470 also inhibited T-loop phosphorylation and activation of Akt, but was more efficient at inhibiting Akt in response to stimuli such as serum that activated the PI3K (phosphoinositide 3-kinase) pathway weakly. GSK2334470 inhibited activation of an Akt1 mutant lacking the PH domain (pleckstrin homology domain) more potently than full-length Akt1, suggesting that GSK2334470 is more effective at inhibiting PDK1 substrates that are activated in the cytosol rather than at the plasma membrane. GSK2334470 also suppressed T-loop phosphorylation and activation of RSK2 (p90 ribosomal S6 kinase 2), another PDK1 target activated by the ERK (extracellular-signal-regulated kinase) pathway^[2]. Furthermore, chemical inhibition of PDK1 using the specific inhibitor GSK2334470 (1 µM) resulted in total abrogation of the EGF-induced intracellular calcium increase and inositol phosphates accumulation in MDA-MB-231 cells^[3].

细胞研究
细胞系	浓度	检测类型	检测时间	活动说明	数据源
F-36P cells		Proliferation assay		Antiproliferative activity against human F-36P cells, IC50=0.28 μM	21341675
insect cells		Function assay		Inhibition of recombinant full length PDK1 (unknown origin) expressed in insect cells assessed as inhibition of Akt activation measured for 30 mins in presence of [gamma32P-ATP], IC50=0.01 μM	23448267
K562 cells		Proliferation assay		Antiproliferative activity against human K562 cells, IC50=18 μM	21341675

实验方案

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.81mL

2.16mL

1.08mL

21.62mL

4.32mL

2.16mL

参考文献

[1]Artamonov M, Momotani K, et al. The p90 ribosomal S6 kinase (RSK) is a mediator of smooth muscle contractility. PLoS One. 2013;8(3):e58703.

[2]Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1

[3]A novel regulatory mechanism links PLCγ1 to PDK1

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靶点

靶点	数值

PDK1	PDK-1, IC50:10 nM