lipid droplets

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

Triacsin C (WS 1228A) from Streptomyces aureofaciens is a differential inhibitor of arachidonic acid coenzyme A synthetase and non-specific long-chain acyl-coenzyme A synthetase, with anti-atherosclerotic activity, inhibition of ACSL activity, and inhibition of the accumulation of TAGs into lipid droplets (LDs).Triacsin C has been used to study rotavirus infection and Alzheimer;s disease. Triacsin C is used to study rotavirus infection and Alzheimer;s disease.

CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LD). It exhibits phototoxicity against breast cancer cells with an IC50 of 0.01-0.02 μM and demonstrates antitumor efficacy in a 4T1 xenograft mouse model.

NUV-244 is a degrader of PNPLA3 I148M. It reduces the levels of PNPLA3 I148M on lipid droplets through BFAR-mediated ubiquitin-proteasome degradation.

NIM-7 is a fluorescent probe, allowing lipid droplets and lysosomes to be labelled simultaneously and with high specificity, being visualized readily through yellow and red fluorescence, using different excitation and detection channels.

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019). MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice. References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019).

ML261 is a inhibitor of hepatic lipid droplets formation with an IC 50 of 69.7 nM. ML261 has research value in non-alcoholic fatty liver disease (NAFLD) and inflammation.

ST-148 maleate, a potent and orally active DENV inhibitor, exhibits antiviral efficacy with low cell toxicity. It disrupts the interaction between lipid droplets and the C protein, inhibiting viral replication. [1]

E722-2648 is a potent inhibitor of the β-catenin BCL9 complex, specifically preventing its formation and inhibiting Wnt activity. It disrupts cholesterol homeostasis through increased cholesterol esterification and accumulation of lipid droplets. Additionally, E722-2648 exhibits antitumor activity [1].

Phenochalasin A (≤ 20 μM) effectively reduces both the quantity and size of lipid droplets in macrophages without exhibiting any cytotoxicity.

Dodoviscin A may be a new promising pigmentation-altering agent for cosmetic and therapeutic applications, it can inhibit melanin biosynthesis induced by 3-isobutyl-1-methylxanthine and PD98059.Dodoviscin A can promote adipocyte differentiation as charact