PIK-93

产品说明书

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Chemical Structure| 593960-11-3 同义名 : -
CAS号 : 593960-11-3
货号 : A764324
分子式 : C14H16ClN3O4S2
纯度 : 98%
分子量 : 389.877
MDL号 : MFCD12922510
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(269.32 mM)，配合低频超声助溶，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
描述 PIK-93 is the first potent, synthetic PI4k inhibitor with IC50 value of 19nM for PI4KIIIb. The inhibition of PI3K by pretreatment of PIK-93 at 300nM for 20min decreased agonist-induced translocation of TRPC6 to the plasma membrane and agonist-induced Ca2+ entry into HEK293 cells. Inhibition of PI4k activity with PIK-93 at 250nM reduced the incidence of DA motor neuron loss and improved backward locomotion in C. elegans with vpr-1 knocked down. Whereas PI4KIIIβ is inhibited by ∼90% at 250nM concentration of PIK93, PI4KIIIα requires >10μM to be inhibited by 50%, and type II PI4Ks are completely resistant to the inhibitor (with purified enzymes tested in vitro in the presence of 100μM ATP). Pretreatment with PIK-93 at 250nM for 10min inhibited the conversion of endogenous ceramide to sphingomyelin in COS-7 cells.
作用机制 PIK93 binds in the ATP-binding pocket of PI4KIIIb.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.82mL

2.56mL

1.28mL

25.65mL

5.13mL

2.56mL
参考文献

[1]Knight ZA, Cell, 2006, 125(4), 733-747.

[2]VanKeymeulen A, et al. Cell Biol. 2006, 174(3), 437-445.