Stearoyl-CoA Desaturase (SCD)

MK-8245 is a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor. MK-8245 is useful for the Treatment of Diabetes and Dyslipidemia.

Selective δ6 desaturase inhibitor (IC50 = 0.2 μM in vitro).

stearoyl-CoA desaturase 1 (SCD1) inhibitor. Used to selectively eliminate undifferentiated human pluripotent stem cells (hPSCs) from culture; induces ER stress, attenuates protein synthesis and induces apoptosis in hPSCs. Prevents teratoma formation in immunocompromised mice.

A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.

MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.

CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).

SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor.

T-3764518 is a novel and potent stearoyl coenzyme A desaturase (SCD) inhibitor with an IC50 of 4.7 nM.

XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.

Aramchol, also known as Arachidyl amido cholanoic acid, is a cholesterol solubilizer that prevents gallstone formation in inbred mice. Aramchol reduces liver fat content in patients with nonalcoholic fatty liver disease.

GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16.

MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an EC50 of 2.3 nM for rSCD1.

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

E6446 is an inhibitor os Toll-like receptor (TLR)7 and 9 signaling.

FASN/SCD-IN-1 is a potent inhibitor of Fatty Acid Synthase (FASN) and Stearoyl-CoA Desaturase (SCD), derived from Silybin. This orally active compound exhibits significant biological activities, including the inhibition of lipid deposition and reduction of FASN and SCD transcription levels. Additionally, FASN/SCD-IN-1 demonstrates antioxidant, anti-inflammatory, and anti-fibrotic properties, with notable hepatoprotective effects in rat models of acute liver injury. Its ability to ameliorate pathological features such as steatosis, inflammation, and fibrosis in mouse models of myeloproliferative steatohepatitis (MASH) makes it a valuable tool for exploring mechanisms underlying MASH-related liver conditions.

SSI-4 is a potent stearoyl-CoA desaturase (SCD1) inhibitor with an EC50 of 1.9 nM for mouse SCD1. By blocking the conversion of saturated fatty acids to monounsaturated fatty acids, SSI-4 effectively reduces oleic and palmitoleic acid production. It promotes lipid peroxidation, induces endoplasmic reticulum stress, and activates apoptotic pathways. Additionally, SSI-4 inhibits mTORC1 activity, suppresses B cell proliferation and antibody production, and induces autophagy. This compound is valuable for studies related to cancers such as acute myeloid leukemia and renal cell carcinoma, as well as influenza infections.

CVT-11127 is a potent inhibitor of stearoyl-CoA desaturase (SCD), which plays a crucial role in lipid metabolism. This compound induces apoptosis and causes cell cycle arrest at the G1/S phase, which may impact cellular proliferation. CVT-11127 is primarily utilized in research related to lung cancer, providing valuable insights into therapeutic strategies targeting SCD pathways.

TPMP-I-2 is an anticancer agent that targets and induces apoptosis in various cancer cell lines while decreasing the protein levels of stearoyl-CoA desaturase. In preclinical studies, TPMP-I-2 has shown efficacy in prolonging survival in nude rats with simulated micrometastatic cervical cancer and effectively reduces tumor growth in breast cancer models when combined with immunotoxins. This compound serves as a valuable tool for researchers investigating novel cancer therapies.

(10E,12Z)-Octadeca-10,12-dienoic acid is a potent PPARα activator that plays a critical role in regulating lipid metabolism and adipocyte differentiation. This compound has demonstrated various biological activities, including antioxidant and antitumor effects, alongside the induction of proinflammatory cytokines and chemokines, which may contribute to decreased adipogenesis and insulin resistance. (10E,12Z)-Octadeca-10,12-dienoic acid also influences milk fat synthesis by reducing the expression of lipogenic enzymes and inhibiting fatty acid desaturation. Additionally, it has been shown to modulate lipoprotein lipase activity in cultured adipocytes and alter hepatic stearoyl-CoA desaturase expression in vivo.

Elemicin is a potent inhibitor of Stearoyl-CoA Desaturase 1 (SCD1), acting through metabolic activation. This compound exhibits a range of biological activities, including anti-influenza, antimicrobial, antioxidant, and antiviral effects. Its mechanism and diverse applications make Elemicin a valuable reagent for research in metabolic studies and infectious disease treatment. Caution is advised, as Elemicin and its reactive metabolite, 1′-Hydroxyelemicin, may induce hepatotoxicity.

SNX7 is a selective inhibitor of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. This compound plays a crucial role in studying cellular senescence and various CDKI-related diseases. By targeting the CDKI pathway, SNX7 serves as a valuable tool in cancer research and other conditions where cell cycle regulation is disrupted.

PFM046 is a potent antagonist of the liver X receptors (LXRα and LXRβ), demonstrating IC50 values of 2.04 μM and 1.58 μM, respectively. This compound effectively inhibits the expression of stearoyl-CoA desaturase 1 (SCD1) and fatty acid synthase (FASN), while promoting the expression of ATP-binding cassette transporter A1 (ABCA1). PFM046 has shown promising antitumor efficacy in preclinical mouse models, making it a valuable tool for research in cancer therapeutics and lipid metabolism pathways.

18:0 Coenzyme A (triammonium) is a substrate for stearoyl-CoA desaturases (SCDs), enzymes that catalyze the desaturation of saturated fatty acids. This compound plays a crucial role in lipid metabolism and is significant in studies focused on fatty acid synthesis and oxidation. It is widely used in research applications investigating metabolic disorders and adipocyte differentiation.

Sterculic acid is a selective inhibitor of stearoyl-CoA desaturase-1 (SCD1), targeting the delta-9 desaturase (Δ9D) activity. It demonstrates significant inhibitory potency with an IC50 value of 0.9 μM. This compound is useful in studies exploring metabolic disorders, lipid metabolism, and the role of SCD1 in various disease states.

SCD1 inhibitor-4 is a selective inhibitor of stearoyl-CoA desaturase-1 (SCD1) with potent oral bioavailability. This compound is primarily utilized in research focused on metabolic disorders, particularly in the study of diabetes. Its ability to modulate lipid metabolism makes it a valuable tool for investigating the role of SCD1 in adipogenesis and insulin sensitivity.

YTX-465 is a potent inhibitor of stearoyl-CoA desaturase (Ole1/SCD), demonstrating IC50 values of 0.039 μM for Ole1 and 30.4 μM for SCD1. This compound is instrumental in studying the biochemical pathways involved in Parkinson's disease and other synucleinopathies. Its ability to modulate Ole1 and SCD1 activity enables a deeper investigation into lipid metabolism and its implications in neurodegenerative conditions.

T-3364366 is a reversible, slow-binding inhibitor of delta-5 desaturase (D5D) with sub-nanomolar potency, showing IC50 values of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cell lines, respectively. This compound demonstrates significant inhibitory activity towards D5D (IC50 = 19 nM) while exhibiting excellent selectivity against delta-6 desaturase (D6D, IC50 = 6200 nM) and stearoyl-CoA desaturase (SCD, IC50 > 10000 nM). T-3364366 serves as a valuable tool for research into lipid metabolism and related disorders.

SCD1/5-IN-1 is a selective inhibitor of stearoyl-CoA desaturase 1 and 5 (SCD1/5), which plays a critical role in lipid metabolism and fatty acid desaturation. This compound demonstrates potential biological activity in modulating lipid profiles and influencing cellular signaling pathways associated with various neurological diseases. SCD1/5-IN-1 is suitable for studies aimed at elucidating the role of SCD enzymes in neurological pathologies and metabolic disorders.

SCD1 Inhibitor-3 is a potent and orally bioavailable inhibitor of stearoyl-CoA desaturase 1 (SCD1). This compound demonstrates significant efficacy in modulating lipid metabolism, making it valuable in the study of metabolic disorders such as obesity, type II diabetes, and dyslipidemia. Additionally, SCD1 Inhibitor-3 may have applications in researching skin conditions, including acne and certain cancers, by influencing cellular lipid profiles.

Cbz-L-Trp-OH is a competitive inhibitor of stearoyl-CoA desaturase (SCD), exhibiting an IC50 of 2.5 μM and a Ki of 2.1 μM. This compound is valuable for studying lipid metabolism and exploring therapeutic interventions in metabolic disorders. Its ability to selectively inhibit SCD makes it a useful tool for investigating the role of fatty acid desaturation in various physiological and pathological processes.

SW203668 TFA is an irreversible inhibitor of stearoyl CoA desaturase (SCD), exhibiting an IC50 of 54 nM. By covalently binding to SCD, it effectively depletes unsaturated fatty acids and induces cell death in sensitive cell types, particularly those expressing CYP4F11. This selective cytotoxicity renders SW203668 TFA particularly valuable in the research of non-small cell lung cancer (NSCLC), as it inhibits tumor growth in CYP4F11-expressing xenografts while sparing other cell types. Its unique mechanism makes it a potent tool for studying targeted therapies in cancer treatment.

XEN103 is a selective inhibitor of stearoyl-CoA desaturase 1 (SCD1), exhibiting IC50 values of 14 nM and 12 nM against mouse SCD1 and human SCD1 in HepG2 cells, respectively. This compound plays a significant role in research related to obesity and type 2 diabetes by modulating lipid metabolism. Additionally, XEN103 has been shown to induce sebaceous gland atrophy in murine models, providing further avenues for study in dermatological and metabolic disorders.

SCD1-IN-1 is a selective inhibitor of stearoyl-CoA desaturase 1 (SCD1), with an IC50 value of 5.8 nM. This compound is primarily used in research focused on dermatological conditions, where modulation of fatty acid metabolism may influence disease outcomes. SCD1-IN-1's ability to inhibit SCD1 makes it a valuable tool for studying the underlying mechanisms of skin-related pathologies and potential therapeutic approaches.

SW203668 is an irreversible inhibitor of stearoyl CoA desaturase (SCD) with an IC50 of 54 nM. It covalently binds to SCD, leading to the depletion of unsaturated fatty acids and triggering cell death in sensitive cells. Notably, SW203668's effectiveness is influenced by the expression of CYP4F11, as its active form is generated through demethylation by this enzyme, resulting in selective toxicity towards CYP4F11-expressing non-small cell lung cancer (NSCLC) cells. Additionally, SW203668 has demonstrated the ability to inhibit tumor growth in immunodeficient mice with NSCLC xenografts while sparing CYP4F11-lacking cells and mouse skin sebocytes, making it a valuable tool for research on non-small cell lung cancer.

MK-8245 analog is a potent inhibitor of stearoyl-CoA desaturase (SCD), exhibiting an IC50 of 7 nM in rat SCD assays. This compound demonstrates significant antidiabetic and antidyslipidemic activities, making it a valuable tool for research in metabolic disorders. Its mechanism of action provides opportunities for investigating SCD-related pathways in various biological contexts.

Cbz-D-Trp-OH is a competitive inhibitor of stearoyl-CoA desaturase (SCD), demonstrating an IC50 of 86 μM and a Ki value of 71 μM. This compound modulates lipid biosynthesis and is instrumental in studying lipid metabolism and related metabolic disorders. Its use is pertinent in research focused on understanding the role of SCD in obesity, diabetes, and cardiovascular diseases.

SCD1 inhibitor-5 is a selective inhibitor of stearoyl-CoA desaturase-1 (SCD1), exhibiting IC50 values of 0.13 μM in H2122 cells and 31 μM in H1819 cells. This compound effectively reduces SCD1 activity, making it a valuable tool in cancer research. Its inhibition of lipid metabolism pathways can provide insights into tumor growth and proliferation mechanisms.

Stearoyl coenzyme A lithium is an active compound utilized as a substrate for the enzymatic activity of stearoyl-CoA desaturase in microsomal preparations. This reagent is important for studying lipid metabolism, particularly in the context of fatty acid desaturation processes. Applications include exploring the role of stearoyl-CoA desaturase in cellular function and investigating related metabolic pathways in biochemical research.

1-Methyl-1H-pyrazole-3-carboxylic acid serves as an intermediate in the synthesis of SCD1 and SCD5 inhibitors. This compound is instrumental in investigating metabolic disorders and their mechanisms. Its role in the development of targeted therapies makes it a valuable reagent for chemical research in metabolic pathways.

PF-244 is a drug derivative that functions as a selective inhibitor of stearoyl-CoA desaturase (SCD). This compound demonstrates significant biological activity by modulating lipid metabolism and may influence cellular processes related to insulin sensitivity and obesity. PF-244 is commonly utilized in research applications focused on metabolic disorders and provides valuable insights into lipid-related pathophysiology.