phospholipase a-1

Desonide (Prednacinolone) 是一种非氟化皮质类固醇抗炎剂，能够作用于糖皮质激素受体。

1-Naphthaleneacetic acid potassium salt (1-NAA Potassium Salt) 是一种合成的植物生长素，能够促进植物生长，也是一种PLA2抑制剂，IC50=13.16 μM。

CCR1 5 8 activator 1 是胞质磷脂酶 A 抑制剂，具有抗真菌活性。

1-Naphthaleneacetic acid (Transplantone) 是一种 PLA2抑制剂，IC50=13.16 μM。它也是一种合成的植物生长素，可以促进植物生长。

Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物，有抗炎、抗氧化和神经保护等作用。

Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。

U-73343 是一种 U-73122 的无活性类似物，能够剂量依赖性的抑制酸分泌，可作为 U-73122 的阴性对照。其中 U 73122 是一种有效的磷脂酶 C (phospholipase C) 和 5-脂氧合酶 (5-LO (5-lipoxygenase)) 抑制剂，对磷脂酶 C 的 IC50值约为 1-2.1 µM。

VU0285655-1(BML-280) 是一种有效的选择性磷脂酶 D2 (PLD2) 抑制剂，可抑制PLD2 缺陷细胞的增殖。VU0285655-1 对高糖诱导的 caspase-3 裂解和细胞活力降低有抑制作用。VU0285655-1 可用于研究糖尿病视网膜病。

DHPG ((RS)-3,5-DHPG) 是一种氨基酸，是选择性代谢型谷氨酸受体 mGluR 的激动剂，也是与磷脂酶 D 耦合的 mGluR 的有效拮抗剂。

ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor. With an IC50 of ~34 μM[1].

PNPLA3 modifier 1 (compound 10) 是针对 patatin 样磷脂酶结构域的蛋白 3 (pnpla3) 的一种修饰剂，具有 4.9 nM 的 EC50 值。

08:0 Lyso PC (1-Octanoyl-sn-glycero-3-phosphocholine) 是一种溶血卵磷脂，能够被磷脂酶 A2 水解。

Anti-Inflammatory Peptide 1 Acetate 在体内具有有效的抗炎活性，是磷脂酶 A2 (PLA2) 的强抑制剂，其存在和活性增加会导致某些身体部位的炎症和疼痛。

Luffariellolide 是一种从海洋海绵 Hyrtios communis中获取的萜烯化合物，是人滑膜蛋白磷脂酶A2 (HSF-PLA2) 抑制剂，也是视黄酸受体（RAR） 激动剂。Luffariellolide 抑制缺氧 （1% O2） 诱导的 HIF-1 激活，抑制细胞生长。

OBAA 是一种有效的磷脂酶 A2 (PLA2) 抑制剂(IC50= 70 nM)，并且在布氏锥虫中阻断 Melittin 诱导的 Ca2+流入(IC50= 0.4 μM)。

FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits glucose-induced increases in prostaglandin E2 production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.

D-myo-Inositol-4-phosphate (Ins(4)P1) is a member of the inositol phosphate (InsP) molecular family that play critical roles as small, soluble second messengers in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3, is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-diphosphate. Binding of Ins(1,4,5)P3 to its receptor on the endoplasmic reticulum results in opening of the calcium channels and an increase in intracellular calcium. Ins(4)P1 can be formed by dephosphorylation of Ins(1,4)P2 by inositol polyphosphate 1-phosphatase or dephosphorylated to inositol by inositol monophosphatase.

PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2References1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitochondria by a stable free-radical prostaglandin polymer (PGBΧ). Proceedings of the National Academy of Sciences of the United States of America 76, 1598-1602 (1979).2. Kumashiro, R., Devlin, T.M., Kholoussy, A.M., et al. Prostaglandin BΧ in the prevention of stress ulcers in rats. International Surgery 70, 247-250 (1985).3. Franson, R.C., Rosenthal, M.D., and Regelson, W. Mechanism(s) of cytoprotective and anti-inflammatory activity of PGB1 oligomers: PGBx has potent anti-phospholipase A2 and anti-oxidant activity. Prostaglandins, Leukotrienes and Essential Fatty Acids 43, 63-70 (1991). PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2 References1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitochondria by a stable free-radical prostaglandin polymer (PGBΧ). Proceedings of the National Academy of Sciences of the United States of America 76, 1598-1602 (1979).2. Kumashiro, R., Devlin, T.M., Kholoussy, A.M., et al. Prostaglandin BΧ in the prevention of stress ulcers in rats. International Surgery 70, 247-250 (1985).3. Franson, R.C., Rosenthal, M.D., and Regelson, W. Mechanism(s) of cytoprotective and anti-inflammatory activity of PGB1 oligomers: PGBx has potent anti-phospholipase A2 and anti-oxidant activity. Prostaglandins, Leukotrienes and Essential Fatty Acids 43, 63-70 (1991).

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) containing C8:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacyl glycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog, compared to naturally-occurring PtdIns, gives it different physical properties including high solubility in aqueous media. PtdIns are phosphorylated to mono- (PtdIns-P; PIP), di- (PtdIns-P2; PIP2), and triphosphates (PtdIns-P3; PIP3). Hydrolysis of PtdIns-(4,5)-P2 by phosphoinositide (PI)-specific phospholipase C generates inositol triphosphate (IP3) and DAG which are key second messengers in an intricate biochemical signal transduction cascade.

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking. PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) is a synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacylglycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog give it different physical properties from naturally-occurring PIP3, including higher solubility in aqueous media.

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(4)-P1 (1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) featuring C8:0 fatty acids at the sn-1 and sn-2 positions. The compound contains the same inositol and diacylglycerol (DAG) stereochemistry as the natural compound. PtdIns-(4)-P1 can be phosphorylated to di- (PtdIns-P2; PIP2) and triphosphates (PtdIns-P3; PIP3). Hydrolysis of PtdIns-(4,5)-P2 by phosphoinositide (PI)-specific phospholipase C generates inositol triphosphate (IP3) and DAG which are key second messengers in an intricate biochemical signal transduction cascade.

D-myo-Inositol-1,3-phosphate (Ins(1,3)P) is a member of the inositol phosphate (InsP) molecular family that play critical roles as small, soluble second messengers in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3 is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. Binding of Ins(1,4,5)P3 to its receptor on the endoplasmic reticulum results in opening of the calcium channels and an increase in intracellular calcium. Ins(1,3)P2 can be dephosphorylated to Ins(1)P by inositol polyphosphate 3-phosphatase and further dephosphorylated to inositol by inositol monophosphatase.

Phosphatidylcholine (PC) species are a common class of phospholipids that comprise the mammalian cell membrane. 1,2-Dioctanoyl PC is a synthetic analog of natural phosphatidylcholine species containing saturated C8:O fatty acids in the sn-1 and sn-2 positions of the glycerol backbone. It exhibits a critical micelle concentration (CMC) value of 0.25 mM at 27°C. 1,2-Dioctanoyl PC serves as an efficient substrate for phospholipase D (PLD) as well as sPLA2 isozymes from bovine pancreas and bee venom.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.