所有图片(1)
别名:
4-氟-N-（2-（4-（5-氟-1H-吲哚-1-基）哌啶-1-基）乙基）苯甲酰胺, 5-氟-2-吲哚脱氯卤派米盐酸盐水合物
经验公式（希尔记法）:
C23H24FN5O2·HCl · xH2O
CAS号:
分子量:
457.93 (anhydrous basis)
MDL编号:
UNSPSC代码:
12352204
PubChem化学物质编号:
NACRES:
NA.77
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质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
颜色
off-white
溶解性
DMSO: >20 mg/mL
储存温度
2-8°C
SMILES字符串
O.Cl.Fc1ccc2[nH]c(cc2c1)C(=O)NCCN3CCC(CC3)N4C(=O)Nc5ccccc45
InChI
1S/C23H24FN5O2.ClH.H2O/c24-16-5-6-18-15(13-16)14-20(26-18)22(30)25-9-12-28-10-7-17(8-11-28)29-21-4-2-1-3-19(21)27-23(29)31;;/h1-6,13-14,17,26H,7-12H2,(H,25,30)(H,27,31);1H;1H2
InChI key
ZORDQKCXPCXYKL-UHFFFAOYSA-N
应用
FIPI（4-氟-N-（2-（4-（5-氟-1H-吲哚-1-基）哌啶-1-基）乙基）苯甲酰胺，5-氟-2-吲哚基脱氯卤代酰亚胺）用于研究依赖于磷脂酶 D1 (PLD1) 和磷脂酶 D2 (PLD2) 活性的细胞信号通路、细胞过程和细胞失调。 FIPI 可用于帮助鉴定和表征磷脂酶 D。
生化/生理作用
FIPI 是一种强效磷脂酶 D (PLD) 抑制剂，在亚 nM 水平下有效。磷脂酶 D (PLD) 和由 PLD 产生的脂类第二信使磷脂酸 (PA) 参与许多细胞生物学过程，包括 Ras 激活、细胞扩散、应力纤维形成、趋化和膜囊泡运输。FIPI 同时抑制 PLD1 和 PLD2，迅速阻断 体内 PA 的生成。FIPI 抑制 PLD 调控 F-肌动蛋白细胞骨架重组、细胞扩散和趋化，显示其具有治疗自身免疫性疾病和癌症转移的潜力。
FIPI 是一种有效的磷脂酶 D (PLD) 抑制剂。信号酶磷脂酶 D (PLD) 和由 PLD 产生的脂类第二信使磷脂酸 (PA) 涉及许多细胞生物学过程，包括 Ras 激活、细胞扩散、应力纤维形成、趋化和膜囊泡运输。FIPI 在体内是 PLD1 和 PLD2 的强效抑制剂，为探索和验证哺乳动物 PLD 的细胞生物学作用奠定了基础。它以低于 nM 的效价快速阻断体内 PA 生成。FIPI 抑制 PLD 调节 F-actin 细胞骨架重组、细胞扩散和趋化，表明其作为自身免疫和癌症转移治疗的潜在效用。它不影响 PLD 亚细胞定位、PIP2 可用性、静息 CHO 细胞中的肌动蛋白应力纤维网络或 PLD 活化近端选择的信号事件。
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Rebecca Elizabeth Kattan et al.
Molecular & cellular proteomics : MCP, 21(2), 100195-100195 (2022-01-11)
Mammalian phospholipase D (PLD) enzyme family consists of six members. Among them, PLD1/2/6 catalyzes phosphatidic acid (PA) production, while PLD3/4/5 has no catalytic activities. Deregulation of the PLD-PA lipid signaling has been associated with various human diseases including cancer. However
My career as a cardiologist and the developmental history of coronary intervention in Japan.
Masakiyo Nobuyoshi
Cardiovascular intervention and therapeutics, 25(2), 51-52 (2010-07-01)
Pablo Lazcano et al.
The Journal of biological chemistry, 298(9), 102363-102363 (2022-08-14)
Inositol is an essential metabolite that serves as a precursor for structural and signaling molecules. Although perturbation of inositol homeostasis has been implicated in numerous human disorders, surprisingly little is known about how inositol levels are regulated in mammalian cells.
David Stegner et al.
Arteriosclerosis, thrombosis, and vascular biology, 33(9), 2212-2217 (2013-07-23)
We recently showed that mice lacking the lipid signaling enzyme phospholipase (PL) D1 or both PLD isoforms (PLD1 and PLD2) were protected from pathological thrombus formation and ischemic stroke, whereas hemostasis was not impaired in these animals. We sought to
Han Han et al.
Molecular cell, 72(2), 328-340 (2018-10-09)
The Hippo pathway plays a crucial role in organ size control and tumor suppression, but its precise regulation is not fully understood. In this study, we discovered that phosphatidic acid (PA)-related lipid signaling is a key regulator of the Hippo
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