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PIK-93

PIK-93 是一种合成的PI4KIIIβ抑制剂，IC50值为 19 nM，同时可抑制PI3Kγ和PI3Kα的活性，IC50值分别为 16 nM 和 39 nM。

CAS号

593960-11-3

分子式

C14H16ClN3O4S2

主要靶点

ATM/ATR|DNA-PK|Carbonic Anhydrase|PI4K|PI3K|HSV|mTOR|Virus Protease

仅限科研使用

Cat No : CM05985

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Synonyms

PIK 93

验证数据展示

  • CAS No.: 593960-11-3

    PIK-93
    CAS#: 593960-11-3

产品信息

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

CAS号 593960-11-3
分子式 C14H16ClN3O4S2
主要靶点 ATM/ATR|DNA-PK|Carbonic Anhydrase|PI4K|PI3K|HSV|mTOR|Virus Protease
主要通路 微生物学|PI3K/Akt/mTOR信号通路|DNA损伤和修复|代谢
分子量 389.88
纯度 99.83%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 PIK 93

靶点活性

PI3Kα:39 nM|PI4K:19 nM

体内活性

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。

溶解度

DMSO:39 mg/mL (100 mM)

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.Knight ZA, Cell, 2006, 125(4), 733-747.
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.Monet M, et al. J BiolChem, 2012, Epub ahead of print.
5.Arita M, et al. J Virol, 2011, 85(5), 2364-2372.

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