fatty acid-binding protein

BMS309403 是有效的、选择性脂肪细胞脂肪酸结合蛋白 aFABP 抑制剂。它可改善载脂蛋白 E 缺乏症小鼠和培养的人内皮细胞的内皮功能。它能够与蛋白质内部的脂肪酸结合口袋相互作用，竞争性地抑制内源性脂肪酸的结合。

STK-15 可作为脂肪酸结合蛋白 5 （FABP5） 抑制剂的候选化合物。

Rimiducid 是一种可渗透脂质的他克莫司类似物，是一种二聚剂，通过交联 FKBP 结构域起作用。它将 Caspase 9 自杀开关二聚化并迅速诱导细胞凋亡。

HTS01037 is an inhibitor of fatty acid-binding. HTS01037 is a competitive antagonist of protein-protein interactions mediated by AFABP aP2 (Ki: 0.67 μM).

Nicodicosapent is a fatty acid niacin conjugate. It is also an inhibitor of the sterol regulatory element-binding protein (SREBP). The sterol regulatory element-binding protein (SREBP) is a key regulator of cholesterol metabolism proteins such as PCSK9, H

BMS-480404 is an effective small molecule inhibitor, which can bind to human keratinocyte fatty acid-binding protein.

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.

LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM[1]. Ki: 0.29 μM (FABP4), 1.3 μM (FABP3)[1]Kd: 2.05 μM (FABP4)[1] LDN 0088050 significantly inhibits LPS-induced expression of both TNFα and IL-6 in RAW264.7 cells[1]. [1]. Zhou Y, et al. The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation. Bioorg Med Chem. 2016 Sep 15;24(18):4310-4317.

FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999

Sodium palmitate-13C is the 13C-labeled variant of palmitic acid, a long-chain saturated fatty acid prevalent in animals and plants. This compound has been shown to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells.

Palmitic acid-13C16 sodium, a 13C-labeled form of the naturally occurring saturated fatty acid Palmitic acid sodium, is prevalent in animals and plants. This compound can trigger the expression of glucose-regulated protein 78 (GRP78) and CCAAT enhancer binding protein homologous protein (CHOP) in mouse granulosa cells.

Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.

BMS-309403 sodium 是一种有效的选择性脂肪细胞脂肪酸结合蛋白aFABP, 也称为FABP4，aP2抑制剂，对 FABP4，FABP3 和 FABP5 的Ki 分别为 <2 nM，250 nM，350 nM。BMS-309403 sodium 与蛋白质内部的脂肪酸结合口袋相互作用，竞争性地抑制内源性脂肪酸的结合。BMS-309403 sodium 可改善载脂蛋白E 缺乏症小鼠和培养的人内皮细胞的内皮功能。

STK-22 is a novel Fatty Acid Binding Protein 5 (FABP5) Inhibitor.

PSB-17365 is a potent GPR84 agonist. PSB-17365 exhibits EC50 values vs. GPR84 of 2.5nM in a cAMP accumulation assay, and 100nM in a β-arrestin 2 recruitment assay. No direct binding affinities are provided. PSB-17365 is selective for GPR84 compared to other free fatty acid receptors (FFAR1 and FFAR4). GPR84, a Gi protein-coupled receptor that is activated by medium-chain (hydroxy)fatty acids, appears to play an important role in inflammation, immunity, and cancer.

DHA-paclitaxel, also know as Taxoprexin, is prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). DHA-paclitaxel exhibits improved pharmacokinetic and toxicity profiles when compared to conventional paclitaxel and has demonstrated antineoplastic activity in animal models of cancer.

Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化，促进肿瘤抑制基因CCAAT 增强子结合蛋白δ (C EBPδ)的重新表达，并通过H-RAS内含子1 CpG岛的去甲基化，激活U937白血病细胞中RAS ERK C EBPβ途径。此外，该化合物能够促进血管平滑肌细胞松弛和血管舒张。

CooP为一种针对线性胶质母细胞瘤的九肽，与胶质母细胞瘤细胞及其相关血管系统中的乳腺来源生长抑制剂 脂肪酸结合蛋白3 (FABP3) 发生结合。该化合物主要应用于化学疗法和多种纳米粒子的靶向递送。

Palmitic acid calcium，一种长链饱和脂肪酸，广泛存在于动物和植物中。它能在小鼠颗粒细胞诱导葡萄糖调节蛋白78 (GRP78) 和CCAAT 增强子结合蛋白同源蛋白 (CHOP) 的表达，可用于建立细胞脂肪变性模型。

1,2-Dipalmitoyl-3-Octanoyl-rac-glycerol 是一种三酰基甘油，其结构特征在于 sn-1 和 sn-2 位置上连接有棕榈酸，在 sn-3 位置上连接有辛酸。棕榈酸，一种广泛存在于动植物体中的长链饱和脂肪酸，已知能够在小鼠颗粒细胞中诱导葡萄糖调节蛋白 78 (GRP78) 与 CCAAT 增强子结合蛋白同源蛋白 (CHOP) 的表达。辛酸，作为一种具有微弱腐臭味的油性液体，不仅应用于酯类香料与染料的制备中，还被认为是一种有效的震颤抑制剂。