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SCD inhibitors block stearoyl-CoA desaturase, the enzyme that makes monounsaturated fatty acids. Stearoyl-coenzyme A desaturase (SCD) inserts a cis double bond at the delta-9 position of palmitoyl-CoA and stearoyl-CoA. Its products, palmitoleate and oleate, are built into triglycerides, phospholipids and cholesteryl esters. In 2002, mice lacking SCD1 were shown to be protected against adiposity, which drew interest to the enzyme in metabolic research. A 2015 X-ray structure of mouse SCD1 showed how this membrane enzyme holds its acyl-CoA substrate. A939572, CAY10566 and XEN723 are SCD1 inhibitors, and MK-8245 was designed to act mainly in the liver. SC-26196 inhibits delta-6 desaturase instead, a related fatty acid desaturase.
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.
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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.
Synonyms: Stearoyl-CoA lithium
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.
