ipla2

MAFP (Methyl Arachidonyl Fluorophosphonate) 是选择性，针对活性位点，不可逆的 cPLA2 和 iPLA2 抑制剂。 MAFP 也是一种有效的不可逆的 anandamide amidase 抑制剂。

(R)-Bromoenol lactone 是不可逆、手性、机理依赖性的 iPLA2γ 抑制剂，对人重组 iPLA2γ 的 IC50 约为 0.6 µM 。

GK187 是一种具有选择性和高效性的 Group VIA 钙非依赖性磷脂酶A2 (GVIA iPLA2) 抑制剂，可用于研究神经系统疾病。

Anti-PLA2G1B Antibody 是一种针对PLA2G1B的CHO表达的人源抗体，带有huIgG1型重链和huκ型轻链，预测分子量 (MW) 为150 kDa。其同型对照可参考HumanIgG1kappa, Isotype Control。

FKGK11 is a potent inhibitor of GVIA iPLA2.

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.

Arachidonoyl Thio-PC is a substrate for many phospholipase A2s (PLA2s) including sPLA2, cPLA2, and iPLA2. Cleavage of the sn-2 fatty acid by PLA2 results in generation of a free thiol which reacts with chromogenic reagents such as DTNB (Ellman's reagent) and DTP to allow quantitation of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by excluding or inhibiting sPLA2 and iPLA2 activities in the assay.

(S)-Bromoenol lactone是一种手性、基于机制的不可逆抑制剂，靶向钙非依赖性磷脂酶A2（iPLA2）。相较其对映体(R)-BEL，(S)-Bromoenol lactone对iPLA2γ（Group VIB）具有更高选择性，并常与(R)-BEL配合使用，以区分iPLA2不同亚型在花生四烯酸释放及细胞信号转导中的功能作用。

GSK563 is a potent GVIA iPLA2 inhibitor (XI(50) 0.0000021, IC50 1 nM). GSK563 is 22 000 times more active against GVIA iPLA2 than GIVA cPLA2. It was found to reduce β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes.

GK563是一种针对Ca2+-independent phospholipase A2(GVIA iPLA2)的选择性抑制剂，具有1 nM的IC50值。相比于GIVA cPLA2，GK563对GVIA iPLA2的抑制活性高出22000倍。它能减少促炎细胞因子诱导的β-cell凋亡，从而增加了其在对抗自身免疫性疾病（例如1型糖尿病）中的潜在应用价值。