lipid droplet

1. Agrimol B is a main active ingredient isolated from Agrimonia pilosa Ledeb.

CAY10650 is an effective inhibitor of cytosolic phospholipase A2α (cPLA2α, IC50: 12 nM).

Beauveriolide III, a cyclodepsipeptide found in Beauveria fungi, inhibits lipid droplet formation (at 3-10 μM) and cholesterol synthesis (IC50=0.41 μM). This compound also suppresses acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity (IC50=5.5 μM) and reduces atherosclerotic lesion size in Ldlr-/- and ApoE-/- mouse models (25-50 mg/kg).

Bafilomycin B1 is a macrolide antibiotic discovered in Streptomyces gresuis. It exhibits neuroprotective effects and V-ATPase inhibitory activity, and can also inhibit LDL-induced lipid droplet accumulation.

Lipophagy inducer 1 (Compound 2726.007) is an agent that induces lipophagy. It primarily acts to reduce lipid droplet accumulation and prevent podocyte death. The compound operates by activating lipophagy and regulating the LXR signaling pathway. Lipophagy inducer 1 is useful for research into diabetic kidney disease (DKD) and other disorders related to lipid metabolism.

NR4A1 agonist 1 is an NR4A1 agonist with a Ki value of 2.96 μM. It demonstrates significant lipid-lowering activity in 3T3-L1 adipocytes, with an EC50 of 0.13 μM, effectively reducing triglyceride (TG) accumulation and lipid droplet formation. NR4A1 agonist 1 is applicable in obesity-related research.

WML-01 is a fungicide with EC50 values of 0.079 μg/mL, 0.72 μg/mL, and 2.02 μg/mL against F. graminearum, F. fujikuroi, and S. sclerotiorum, respectively. It disrupts the cell membrane of F. graminearum and induces lipid droplet deposition. WML-01 inhibits the biosynthesis of deoxynivalenol (DON) without cross-resistance and significantly impedes the assembly of ribosomal subunits, thereby hindering protein synthesis. WML-01 effectively controls the spread of Fusarium head blight (FHB) in wheat.

Sino-C is a Sinomenine derivative with anticancer properties. It disrupts cholesterol homeostasis by upregulating crucial genes such as SREBF2 and HMGCS1, leading to intracellular cholesterol accumulation and lipid droplet formation. The metabolic disturbance induced by Sino-C further triggers lipid peroxidation and endoplasmic reticulum (ER) stress, initiating a unique mixed form of cell death that includes both apoptotic (cleaved PARP) and necrotic-like features. Sino-C is applicable in studies of colorectal cancer, lung cancer, and breast cancer.

ASK1-IN-12 is an ASK1 inhibitor with an IC50 of 6.3 nM. It effectively suppresses the activation of the ASK1-p38/JNK pathway induced by TNF-α. Additionally, ASK1-IN-12 reduces cholesterol elevation and lipid droplet accumulation induced by free fatty acids, improving hepatic steatosis. This compound is valuable for research on non-alcoholic steatohepatitis (NASH).

ISR activator 3 (Compound cc81) is the active metabolite of A8. It activates the integrated stress response (ISR) by binding to RIG-I (KD≈ 0.55 μM) without inducing lipid droplet clearance. Additionally, ISR activator 3 enhances the interferon response under viral mimic signaling. This compound is applicable in studies of neurodegenerative diseases and immune stress.

E722-2648 TFA is an effective inhibitor of the β-catenin/BCL9 complex. It specifically restricts the formation of the β-catenin/BCL9 complex and inhibits Wnt activity. By enhancing cholesterol esterification and lipid droplet accumulation, E722-2648 TFA disrupts cholesterol homeostasis. This compound also exhibits antitumor activity.

OB-1 is a protein-like protein-3 (STOML3) inhibitor, inhibiting adipogenesis and lipid droplet growth by downregulating the PPARγ pathway. OB-1 inhibits adipogenesis and lipid droplet growth by interfering with the self-association of stomatin.

1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fasting alter hepatic lipid droplet proteome and diacylglycerol species and prevent diabetes in NZO mice. Biochim. Biophys. Acta 1851(5), 566-576 (2015).2. Narváez-Rivas, M., Vicario, I.M., Constante, E.G., et al. Changes in the concentrations of free fatty acid, monoacylglycerol, and diacylglycerol in the subcutaneous fat of Iberian ham during the dry-curing process. J. Agric. Food Chem. 55(26), 10953-10961 (2007). 1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2 References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fasting alter hepatic lipid droplet proteome and diacylglycerol species and prevent diabetes in NZO mice. Biochim. Biophys. Acta 1851(5), 566-576 (2015).2. Narváez-Rivas, M., Vicario, I.M., Constante, E.G., et al. Changes in the concentrations of free fatty acid, monoacylglycerol, and diacylglycerol in the subcutaneous fat of Iberian ham during the dry-curing process. J. Agric. Food Chem. 55(26), 10953-10961 (2007).

ML-262 is an effective inhibitor of hepatic lipid droplet formation and is used in studies of non-alcoholic fatty liver disease.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Curcumin 5-8 (CUR5-8), a naturally active analog of curcumin (CUR), exhibits potent oral activity. It effectively inhibits lipid droplet formation, enhances autophagy, and reduces apoptosis. Additionally, Curcumin 5-8 has been shown to ameliorate insulin resistance and enhance insulin sensitivity [1].

Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.

1-Linoleoyl-2-oleoyl-3-stearoyl-rac-glycerol is a triglyceride molecule known for its biological activity in promoting lipid droplet formation. The unique combination of fatty acids in 1-Linoleoyl-2-oleoyl-3-stearoyl-rac-glycerol makes it a valuable tool for studying the roles of fatty acids. It finds extensive application in cell biology and metabolic research.

IRW is an orally active tripeptide extracted from egg whites with angiotensin-converting enzyme (ACE) inhibitory properties. It helps prevent non-alcoholic fatty liver disease (NAFLD) induced by a high-fat diet (HFD) through the regulation of hepatic lipid metabolism and increased mitochondrial content. IRW reduces hepatic triglyceride levels and lipid droplet size, and enhances liver mitochondrial complexes, citrate synthase activity, and 5'-AMP-activated protein kinase phosphorylation, along with the abundance of microsomal triglyceride transfer protein. It also increases phosphorylated acetyl CoA carboxylase and mitochondrial complexes, making it useful for inflammation-related research.