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CAS No.: 593960-11-3

PIK-93 Catalog No. CSN17170

Synonyms: N/A

PIK-93 is the potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and shown to inhibit PI3Kα with IC50 of 39 nM.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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.
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5649 mL
- 12.8245 mL
- 25.6491 mL
- 5 mM
- 0.5130 mL
- 2.5649 mL
- 5.1298 mL
- 10 mM
- 0.2565 mL
- 1.2825 mL
- 2.5649 mL

技术信息

CAS号

593960-11-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H16ClN3O4S2

运输

蓝冰

分子量

389.88

别名

N/A

溶解度

DMSO	78.0 mg/mL (200.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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