PPAR

MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).

Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.

Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.

MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects.

Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.

Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research.

MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia.

AZ0108 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), including PARP1, PARP2, PARP3, PARP6, TNKS1, and TNKS2. It displays potent inhibitory activity with IC50 values of <0.03 μM for PARP1 and PARP2, and exhibits significant biological effects such as preventing centrosome clustering with an EC50 of 0.053 μM. Additionally, AZ0108 demonstrates cytotoxicity in OCI-LY-19 cells, with a GI50 value of 0.017 μM, and shows favorable pharmacokinetic properties in rat and mouse models, making it a valuable tool for cellular and molecular biology research focused on DNA repair and cancer therapeutic studies.

AZD-9574-acid is a selective PPAR-1 inhibitor that serves as a crucial building block for the development of PROTAC molecules. Its inhibition of PPAR-1 demonstrates significant potential in the regulation of metabolic pathways and inflammatory responses. This compound is essential for researchers exploring targeted protein degradation and its applications in therapeutic development.

Soyasaponin Ab is a potent PPARγ inhibitor with oral bioavailability. It effectively suppresses PPARγ transcriptional activity and induces apoptosis at elevated concentrations. This compound exhibits a range of biological activities, including anti-obesity, anti-oxidation, anti-inflammation, and anti-aging effects. Additionally, Soyasaponin Ab has been shown to mitigate memory impairment induced by Scopolamine, making it a valuable reagent for research in metabolic and neuroprotective applications.

Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies.

PPARγ-IN-2 is a selective PPARγ inhibitor that effectively reduces triglyceride accumulation in 3T3-L1 preadipocytes, with an EC50 of 0.106 μM. This compound demonstrates potential for mitigating obesity and associated metabolic syndrome, particularly in the context of a high-cholesterol diet. Its ability to diminish lipid accumulation in adipose tissue makes it a valuable tool for research focused on metabolic disorders and adipocyte biology.

SR 16832 is a dual-site covalent inhibitor of peroxisome proliferator-activated receptor gamma (PPARγ). It functions by targeting both orthosteric and allosteric sites, leading to significant modulation of PPARγ activity. This compound is valuable for research applications related to metabolic disorders, obesity, and diabetes, particularly in studies investigating the downstream effects of PPARγ inhibition on gene expression and cellular metabolism.

FTX-6746 is an orally active inhibitor of peroxisome proliferator-activated receptor gamma (PPARG). It demonstrates significant tumor inhibition in mouse xenograft models, making it a valuable tool for investigating the therapeutic potential of targeting PPARG in cancer research. Its specificity and efficacy in modulating PPARG activity support its use in studies related to metabolic disorders and cancer biology.

Netoglitazone is a dual agonist targeting PPARα and PPARγ, exhibiting significant antihyperglycemic activity. This compound is instrumental in metabolic research and provides insights into the regulation of glucose homeostasis. Its application in studies related to diabetes and metabolic syndrome makes it a valuable tool for exploring therapeutic strategies.

trans-Cinnamyl alcohol is a selective PPARγ inhibitor that plays a significant role in regulating lipid metabolism and adipogenesis. As a metabolite derived from chestnut flowers, it exhibits anti-obesity activity by inhibiting PPARγ expression. This compound is valuable for research applications focused on obesity, metabolic disorders, and the modulation of fat cell differentiation.

PPARγ phosphorylation inhibitor 1 is a selective inhibitor targeting Peroxisome Proliferator-Activated Receptor gamma (PPARγ). It effectively inhibits CDK5-mediated phosphorylation of PPARγ at Ser273 with an IC50 of 160 nM, demonstrating a binding affinity with an IC50 of 24 nM. This compound exhibits minimal PPARγ agonistic activity in reporter gene assays, making it a valuable tool for studying the role of PPARγ phosphorylation in metabolic disorders and antidiabetic research applications.

Anti-NASH agent 1 is a potent PPAR-α/δ inhibitor that effectively targets nonalcoholic steatohepatitis (NASH). This compound has demonstrated significant efficacy in improving hyperlipidemia, liver fat degeneration, and liver inflammation in a methionine-choline deficiency (MCD) induced NASH mouse model. Additionally, Anti-NASH agent 1 exhibits low liver toxicity while providing protective effects on liver health, making it a valuable tool for research into metabolic disorders and liver diseases.

Soyasaponin Aa is a PPARγ inhibitor that demonstrates significant anti-obesity effects in 3T3-L1 adipocytes by downregulating the activity of peroxisome proliferator-activated receptor γ. Its biological activity supports research into mechanisms of adipogenesis and metabolic regulation. Soyasaponin Aa is useful in studies aimed at understanding the therapeutic potential of targeting PPARγ in obesity-related conditions.

BGT-002 is a potent dual inhibitor of ATP-citrate lyase (ACLY) and a peroxisome proliferator-activated receptor alpha (PPARα) agonist. This compound effectively reduces lipogenesis by inhibiting fatty acid synthesis and enhancing lipid efflux. BGT-002 has shown efficacy in improving metabolic dysfunction-related steatohepatitis and hyperlipidemia in vivo, making it a valuable reagent for research into hypercholesterolemia and related metabolic disorders.

EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD).

Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury.

PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders.

Timcodar is a selective PPAR inhibitor that effectively blocks adipogenic transcriptional regulators, specifically PPARγ and C/EBPα, thereby reducing fat accumulation. Its mechanism of action mirrors that of rapamycin but without inducing immunosuppression or glucose resistance. Timcodar's significant impact on adipogenesis may offer a promising therapeutic avenue for addressing obesity, a growing global health concern. This compound is ideally suited for research related to metabolic disorders and obesity treatment strategies.

PPARγ-IN-5 is a selective inhibitor of PPARγ, a key regulator of adipocyte differentiation and lipid metabolism. This compound effectively reduces lipid accumulation in hepatocytes, demonstrating minimal cytotoxicity at concentrations up to 400 µM in HepG2 cells. PPARγ-IN-5 is suitable for investigations into non-alcoholic fatty liver disease and related metabolic disorders.

(±)-CBCQ is a potent inhibitor of PPAR-γ, exhibiting an EC50 value of 14.7 μM. This compound is of interest in research investigating the modulation of metabolic pathways and the potential therapeutic effects in obesity and diabetes. Its ability to interact with PPAR-γ makes it a valuable tool for studying the receptor's role in gene expression and lipid metabolism.