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

• 靶點(diǎn)： ATM/ATR;Carbonic Anhydrase;DNA-PK;HSV;mTOR;PI3K;PI4K;Virus Protease;ATM/ATR;DNA-PK;VirusProtease;PI3K;CarbonicAnhydrase;PI4K;mTOR;HSV

• 體外研究：
  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.

• 體內(nèi)研究：
  0.5 μM-1 μM PIK-93作用于分化的HL60細(xì)胞,損害用f-Met-Leu-Phe處理而形成的聚集的穩(wěn)定性。在COS-7細(xì)胞中,PIK-93（250 nM）有效地消除了高爾基體中CERT-PH結(jié)構(gòu)域和FL-Cer的積累。在T6.11細(xì)胞中,300 nM PIK-93降低Carbachol誘導(dǎo)的TRPC6移位到質(zhì)膜上和Ca2+進(jìn)入。相同濃度PIK-93也明顯抑制[3H]絲氨酸標(biāo)記的內(nèi)源性神經(jīng)酰胺轉(zhuǎn)變?yōu)樯窠?jīng)鞘磷脂。這些說明了PI4KIIIβ在內(nèi)質(zhì)網(wǎng)和高爾基體中的神經(jīng)酰胺轉(zhuǎn)移時具有重要作用,以及有效調(diào)節(jié)鞘磷脂的合成。一項研究顯示,PIK-93具有抗腸道病毒功能,抑制脊髓灰質(zhì)炎病毒和丙型肝炎病毒復(fù)制,EC50分別為0.14 μM和1.9 μM。PIK-93有效抑制PI3Kγ和PI4KIIIβ,IC50分別為16 nM和19 nM。PIK-93也抑制其他PI3Ks成員,包括PI3Kα,β和δ,IC50分別為39 nM,0.59 μM和0.12 μM。而PIK-93對其他激酶幾乎沒有抑制效果,即使?jié)舛葹?0 μM

• 細(xì)胞實驗： 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)

• 參考文獻(xiàn)：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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