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• 产品描述： PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.

• 靶点： ATM/ATR;Carbonic Anhydrase;DNA-PK;HSV;mTOR;PI3K;PI4K;Virus Protease;ATM/ATR;DNA-PK;VirusProtease;PI3K;CarbonicAnhydrase;PI4K;mTOR;HSV

• 体外研究：
  PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 μM, and 0.12 μM, respectively. PIK-93 shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 μM. In differentiated HL60 (dHL60) cells, PIK-93 (0.5 μM-1 μM) impairs consolidation and stability of the leading edge formed after treatment with uniform f-Met-Leu-Phe (fMLP). PIK-93 alters the localization, but not the amount, of the fMLP-dependent accumulation of total F-actin. In fMLP gradients, PIK-93 reduces the chemotactic index and triples the cells' turning frequency. In COS-7 cells, PIK-93 (250 nM) effectively abrogates the accumulation of CERT-PH domain and FL-Cer in Golgi. PIK-93 of the same concentration also significantly inhibits the conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin. These facts indicate a key role of PI4KIIIβ in ceramide transport between the ER and Golgi, as well as in the regulation of spingomyelin synthesis. In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry. A recent report shows that PIK-93 has anti-enterovirus effects, as revealed by its inhibition of both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC50 values of 0.14 µM and 1.9 µM, respectively.

• 体内研究：
  0.5 μM-1 μM PIK-93作用于分化的HL60细胞,损害用f-Met-Leu-Phe处理而形成的聚集的稳定性。在COS-7细胞中,PIK-93（250 nM）有效地消除了高尔基体中CERT-PH结构域和FL-Cer的积累。在T6.11细胞中,300 nM PIK-93降低Carbachol诱导的TRPC6移位到质膜上和Ca2+进入。相同浓度PIK-93也明显抑制[3H]丝氨酸标记的内源性神经酰胺转变为神经鞘磷脂。这些说明了PI4KIIIβ在内质网和高尔基体中的神经酰胺转移时具有重要作用,以及有效调节鞘磷脂的合成。一项研究显示,PIK-93具有抗肠道病毒功能,抑制脊髓灰质炎病毒和丙型肝炎病毒复制,EC50分别为0.14 μM和1.9 μM。PIK-93有效抑制PI3Kγ和PI4KIIIβ,IC50分别为16 nM和19 nM。PIK-93也抑制其他PI3Ks成员,包括PI3Kα,β和δ,IC50分别为39 nM,0.59 μM和0.12 μM。而PIK-93对其他激酶几乎没有抑制效果,即使浓度为10 μM

• 细胞实验： For actin staining, dHL60 cells are preincubated in suspension with PIK-93 or vehicle for 40 min, centrifuged for 5 min at 2000 rpm at room temperature in a J6-B centrifuge, resuspended in mHBSS containing the respective agent at the same concentration, allowed to stick to fibronectin-covered coverslips, and subjected to stimulation with a uniform concentration of 100 nM f-Met-Leu-Phe (fMLP) for 3 min. Cellsare fixed in 3.7% PFA and stained with 10 units/mL rhodamine-phalloidin for 15 min.(Only for Reference)

• 参考文献：
  1. Monet M, et al. J BiolChem, 2012, Epub ahead of print. 2. VanKeymeulen A, et al. Cell Biol. 2006, 174(3), 437-445. 3. Tóth B, et al. J BiolChem, 2006, 281(47), 36369-3637 4. Knight ZA, Cell, 2006, 125(4), 733-747. 5. Arita M, et al. J Virol, 2011, 85(5), 2364-2372.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.565 ml	12.824 ml	25.649 ml
  5 mM	0.513 ml	2.565 ml	5.13 ml
  10 mM	0.256 ml	1.282 ml	2.565 ml
  50 mM	0.051 ml	0.256 ml	0.513 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *