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SGK1 Inhibitor
SI-113 is an inhibitor of SGK1, demonstrating an IC50 of 600 nM. This compound is known to induce autophagy, making it a valuable tool for studying cellular mechanisms related to SGK1 activity. It has potential applications in research areas such as cancer biology and neurodegenerative diseases, where modulation of autophagy may be beneficial. -
SGK1 Inhibitor
SGK1-IN-4 is a selective inhibitor of Serum/Glucocorticoid-regulated Kinase 1 (SGK1), demonstrating oral bioactivity. This compound has potential applications in the study of osteoarthritis, targeting pathways involved in inflammation and cellular signaling. Its ability to modulate SGK1 activity makes it a valuable tool for investigating SGK1's role in various biological processes and disease states. -
SGK1 Inhibitor
SGK1-IN-2 is a selective inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1), characterized by an IC50 value of 5 nM at an ATP concentration of 10 μM. This compound effectively regulates SGK1 activity, influencing various cellular processes such as cell survival, proliferation, and metabolism. SGK1-IN-2 is valuable for research applications focused on cancer biology, cardiovascular diseases, and metabolic disorders. -
SGK1 Inhibitor
SGK1-IN-3 is a potent selective inhibitor of SGK1, exhibiting an IC50 of less than 1 μM. This compound demonstrates significant inhibitory activity, making it a valuable tool for investigating the role of SGK1 in various biological processes. Its application in research may provide insights into the mechanisms underlying osteoarthritis and contribute to the development of novel therapeutic strategies. -
SGK1 Inhibitor
SGK1-IN-6 is a selective inhibitor of SGK1, demonstrating a high potency with an IC50 value of 0.39 μM. This compound effectively suppresses tumor growth in the PC3 xenograft model in BALB/c nude mice while exhibiting no significant toxicity. SGK1-IN-6 is ideal for research applications focused on cancer biology and the exploration of SGK1's role in tumorigenesis. -
SGK1 Inhibitor
SGK1-IN-5 is a potent inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with an IC50 of 3 nM. This compound effectively inhibits SGK1-dependent phosphorylation of glycogen synthase kinase 3 beta (GSK3β) in U2OS cells, demonstrating an IC50 of 1.4 μM. SGK1-IN-5 is valuable for research applications related to osteoarthritis and rheumatism, contributing to the understanding of pathways involved in inflammatory and degenerative joint diseases. -
SHMT Inhibitor
(+)SHIN2 is a selective inhibitor of serine hydroxymethyltransferase (SHMT), a key enzyme involved in folate metabolism and one-carbon metabolism. This compound has been shown to enhance survival in mouse models of NOTCH1-driven acute lymphoblastic leukemia (T-ALL) when used in conjunction with Methotrexate. Additionally, (+)SHIN2 features an alkyne group that facilitates its use in click chemistry applications, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
SHMT1/2 Inhibitor
SHMT-IN-2 is a stereospecific inhibitor of human serine hydroxymethyltransferases SHMT1 and SHMT2, exhibiting IC50 values of 13 nM and 66 nM, respectively. This compound effectively inhibits the proliferation of various human cancer cell lines and demonstrates notable sensitivity towards B-cell lymphomas. SHMT-IN-2 serves as a valuable tool for research investigating metabolic pathways involved in cancer cell growth and treatment response. -
SHMT Inhibitor
SHMT-IN-1 is a potent inhibitor of plasmodial serine hydroxymethyltransferase (SHMT). This compound demonstrates significant antitumor activity, making it a valuable tool for research focused on cancer therapeutics and metabolic pathways. Its efficacy in inhibiting SHMT highlights its potential application in the study of malaria and related biological processes. -
SHMT Inhibitor
SHMT-IN-3 is a selective inhibitor of serine hydroxymethyltransferases SHMT1 and SHMT2, with an IC50 of 0.53 µM for human SHMT1. This compound demonstrates noncompetitive inhibition against serine, making it a valuable tool for studying metabolic pathways involving one-carbon metabolism. SHMT-IN-3 is useful for investigating the role of SHMT in various biological processes and may have applications in cancer research and other metabolic disorders. -
SHMT1 Inhibitor
SHMT-IN-4 is an inhibitor of serine hydroxymethyltransferase (SHMT1), demonstrating an IC50 value of 193.8 g a.i./ha. This compound interferes with amino acid synthesis and metabolism in plants by binding to SHMT1, leading to inhibited plant growth. Importantly, SHMT-IN-4 exhibits minimal toxicity to maize and honeybees, making it a viable option for agricultural research applications focusing on selective herbicide development. -
SCD1 Inhibitor
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
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. -
Ole1/SCD Inhibitor
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. -
D5D Inhibitor
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 Inhibitor
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
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. -
SCD Inhibitor
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. -
SCD Inhibitor
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. -
SCD1 Inhibitor
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. -
SCD Inhibitor
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. -
SCD inhibitor
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. -
SCD Inhibitor
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
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. -
STS Inhibitor
Estrone O-sulfamate is a potent inhibitor of steroid sulfatase (STS), a key enzyme involved in steroid hormone metabolism. It demonstrates significant inhibitory activity with IC50 values of 18 nM in placental microsomes and 0.83 nM in MCF-7 cells. This compound is valuable for research focused on cancer, as it helps elucidate the role of STS in tumorigenesis and hormone-driven malignancies. -
Steroid Sulfatase Inhibitor
Estradiol 3-sulfamate is a potent steroid sulfatase inhibitor, effectively targeting estrone sulfatase with an IC50 value of 251 nM and a Ki of 133 nM. This compound is recognized for its long-acting and orally active properties, making it a valuable reagent for research applications focused on hormone metabolism and endocrine signaling. Its ability to modulate sulfated steroid levels supports investigations into various biological processes, including cancer research and reproductive health studies. -
Steroid Sulfatase Inhibitor
KW-2581 is a selective steroid sulfatase (STS) inhibitor, exhibiting an IC50 of 4 nM. This compound effectively inhibits STS activity in ZR-75-1 cells with an IC50 of 13 nM, demonstrating significant impairment of E1S-stimulated cell growth at an IC50 of 0.18 nM. KW-2581 has shown the ability to inhibit sulfated estrogen-dependent proliferation of breast cancer cells both in vitro and in vivo, leading to tumor regression in E1S-induced models. This reagent is suitable for studies focused on hormone receptor-positive breast cancer and the role of steroid sulfatase in tumor biology. -
STS Inhibitor/ERα Modulator
SR-16157 is a dual-action steroid sulfatase (STS) inhibitor and selective estrogen receptor alpha (ERα) modulator, with an IC50 of 0.1 µM. This compound displays potent STS inhibitory and anti-estrogenic effects in breast cancer cells, making it a valuable tool for understanding the role of estrogen signaling in cancer progression. SR-16157 is applicable in breast cancer research, particularly in studies exploring therapeutic strategies targeting estrogen metabolism and receptor modulation. -
Steroid Sulfatase Inhibitor
Steroid sulfatase-IN-10 is a potent inhibitor of steroid sulfatase, exhibiting an IC50 range of 0.03-0.27 µM. This compound is valuable for investigating its role in various inflammatory conditions, including rheumatoid arthritis, type 1 and type 2 diabetes, and systemic lupus erythematosus. Its selective inhibition of steroid sulfatase makes it a useful tool in exploring therapeutic avenues for these diseases. -
Steroid sulfatase/17β-HSD1 Inhibitor
Steroid sulfatase/17β-HSD1-IN-3 is a potent dual inhibitor targeting steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). It irreversibly inhibits human STS activity with an IC50 of 27 nM, demonstrating significant efficacy. This compound is suitable for research focused on endometriosis and other estrogen-dependent diseases, facilitating the exploration of therapeutic strategies in these areas. -
STS Inhibitor
Steroid Sulfatase-IN-2 is a potent steroid sulfatase (STS) inhibitor, exhibiting an IC50 value of 109.5 nM. This compound enables research into hormone-dependent cancers, particularly those driven by estrogen, such as breast and endometrial cancer. Its role as an STS inhibitor makes it a valuable tool for understanding the molecular mechanisms underlying these cancer types and exploring potential therapeutic strategies. -
STS Inhibitor
Steroid sulfatase-IN-8 is a potent steroid sulfatase (STS) inhibitor, demonstrating a pharmacological IC50 of 1 nM in PM models and 0.025 nM in JEG-3 cells. This compound effectively interferes with steroid metabolism, making it a valuable tool for investigating steroid-related pathways. Its application extends to studies on hormone-dependent cancers and other conditions linked to altered steroid levels. -
Steroid Sulfatase Inhibitor
DU-14 is a potent inhibitor of steroid sulfatase, exhibiting an IC50 of 55.8 nM. It effectively reduces MCF-7 cell proliferation, with an IC50 value of 38.7 nM. Additionally, DU-14 demonstrates neuroprotective properties against neurotoxic amyloid-beta (Aβ), indicating its potential to up-regulate endogenous dehydroepiandrosterone sulfate (DHEAS) and alleviate Aβ-induced deficits in spatial memory and synaptic plasticity. This compound is valuable for research in cancer biology and neurodegenerative diseases. -
STS Inhibitor
Steroid sulfatase-IN-4 is an irreversible inhibitor of steroid sulfatase (STS), exhibiting an IC50 of 25 nM against human STS. This compound is primarily utilized in research focused on endometriosis, offering potential insights into the role of STS in disease progression and therapeutic interventions. Its selective inhibition of STS facilitates the exploration of hormonal pathways involved in reproductive health. -
STS Inhibitor
Steroid sulfatase-IN-3 is a potent inhibitor of steroid sulfatase (STS) with an IC50 value of 25.8 nM. This compound exhibits significant antiproliferative activity against T-47D estrogen-dependent breast cancer cells, demonstrating an IC50 of 1.04 µM. Steroid sulfatase-IN-3 is primarily utilized in cancer research to explore the role of STS in hormone-dependent tumor progression and treatment resistance. -
Steroid Sulfatase Inhibitor
Steroid sulfatase-IN-1 is a highly effective inhibitor of steroid sulfatase, exhibiting an IC50 value of 1.71 nM. This compound demonstrates significant antitumor activity in vivo, indicating its potential utility in cancer research. Steroid sulfatase-IN-1 is particularly relevant for studies focused on breast cancer, providing insights into mechanisms of disease and potential therapeutic approaches. -
Steroid sulfatase/17β-HSD1 Inhibitor
Steroid sulfatase/17β-HSD1-IN-1 is a potent inhibitor of steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), exhibiting an IC50 value of 28 nM for human steroid sulfatase in cellular assays. This compound is valuable for investigating estrogen-dependent diseases, making it an important tool for research in hormone-related therapeutic areas. Its specificity and potency support studies aiming to elucidate the role of these enzymes in disease mechanisms. -
Steroid sulfatase/17β-HSD1 Inhibitor
Steroid sulfatase/17β-HSD1-IN-4 is a potent dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). It irreversibly inhibits hSTS activity, demonstrating an IC50 value of 63 nM. This compound is valuable for studying endometriosis and other estrogen-dependent diseases, providing insights into the role of steroid metabolism in these conditions. -
Steroid Sulfatase Inhibitor
Steroid sulfatase-IN-11 is a potent inhibitor of steroid sulfatase, an enzyme that hydrolyzes steroid sulfates. By effectively reducing steroid sulfatase activity, this compound is instrumental in the study of hormone-dependent cancers. Its application in research provides valuable insights into the role of steroid metabolism in cancer progression and therapeutic resistance. -
Succinate Dehydrogenase Inhibitor
Flubeneteram is an inhibitor of succinate dehydrogenase, exhibiting an IC50 value of 0.0484 μM. This compound effectively disrupts the activity of succinate dehydrogenase, contributing to its biological activity. Flubeneteram has demonstrated protective effects against fungal pathogens such as Rhizoctonia solani and Sphaerotheca fuliginea in preclinical studies. It is a valuable reagent for research focused on fungal infection mechanisms and potential therapeutic strategies. -
TrxR Inhibitor
Ethaselen is a selective thioredoxin reductase (TrxR) inhibitor known for its potent inhibitory action, with IC50 values of 0.5 μM for wild-type human TrxR1 and 0.35 μM for rat TrxR1. This organoselenium compound specifically targets the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen demonstrates significant antitumor activity, particularly against non-small cell lung cancer (NSCLC), making it a promising candidate for cancer research applications focused on apoptosis and redox regulation. -
TrxR1 Inhibitor
DVD-445 is a potent peptidomimetic inhibitor of thioredoxin reductase 1 (TrxR1), exhibiting an IC50 value of 0.60 μM against rat TrxR1. This compound demonstrates significant anticancer activity, making it a valuable tool for research applications focused on cancer biology and oxidative stress mechanisms. Its ability to interact covalently with TrxR1 positions DVD-445 as an important reagent for exploring therapeutic strategies targeting oxidative stress in cancer cells. -
TrxR Inhibitor
TrxR-IN-2 is a selective inhibitor of thioredoxin reductase (TrxR), a critical enzyme involved in redox regulation. This compound demonstrates significant inhibitory activity in various cancer models, particularly in drug-resistant hepatocellular carcinoma. TrxR-IN-2 is suitable for research applications focused on understanding TrxR's role in cancer biology and exploring potential therapeutic strategies against aggressive tumor types. -
Trx/TrxR System Inhibitor
PMX464 is a thiol-reactive quinol that acts as an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system. This compound has been shown to inhibit NF-κB-mediated pro-inflammatory activation in human type II alveolar epithelial cells, making it a valuable tool for research focused on inflammation and oxidative stress. PMX464 is particularly useful in studies examining the role of redox signaling in various pathophysiological conditions. -
TrxR Inhibitor
TrxR-IN-3 is a potent inhibitor of thioredoxin reductase (TrxR), exhibiting significant antiproliferative activity against various human cancer cell lines, particularly breast cancer cells. This compound enhances reactive oxygen species (ROS) levels, leading to apoptosis through the modulation of apoptosis-related proteins. Additionally, TrxR-IN-3 promotes autophagy by increasing the expression of LC3-II and Beclin-1 while reducing levels of LC3-I and p62, facilitating the formation of autophagosomes and autolysosomes. This makes TrxR-IN-3 a valuable tool for studying the mechanisms of cancer cell death and autophagy. -
TrxR1 Inhibitor
TrxR1-IN-1 is a selective inhibitor of thioredoxin reductase 1 (TrxR1), exhibiting an IC50 of 8.8 μM. This compound demonstrates significant anticancer activity, achieving IC50 values of 1.5 μM in MCF-7 cells, 1.7 μM in HeLa cells, 2.4 μM in BGC-823 cells, 2.8 μM in SW-480 cells, and 2.1 μM in A549 cells. Additionally, TrxR1-IN-1 possesses antioxidant properties and effectively scavenges DPPH radicals, making it a valuable tool for research in cancer biology and oxidative stress studies. -
TrxR Inhibitor
TrxR-IN-4 is a potent inhibitor of thioredoxin reductase (TrxR), demonstrating significant biological activity by inducing apoptosis in HepG2 cells via the activation of endoplasmic reticulum stress (ERS). This compound also exhibits protective effects against CCl4-induced liver damage in vivo, achieved through the down-regulation of TrxR expression and inflammatory responses. TrxR-IN-4 is a valuable tool for researching the modulation of oxidative stress and cancer therapies. -
TrxR Inhibitor
CPUL1 is a selective inhibitor of thioredoxin reductase (TrxR), demonstrating significant anti-proliferative and anti-metastatic effects in A549 lung cancer cells. It modulates epithelial-mesenchymal transition (EMT) through the induction of reactive oxygen species (ROS) and activation of ERK/JNK signaling pathways resulting from the inhibition of TrxR1 enzyme activity. CPUL1 exhibits enhanced efficacy when used in combination with α-Lipoic Acid or Dithiodipropionic acid, making it a valuable tool for cancer research and therapeutic strategies. -
Tyrosinase Inhibitor
Methyl rosmarinate is a noncompetitive inhibitor of tyrosinase, effectively isolated from Rabdosia serra, with an IC50 value of 0.28 mM for mushroom tyrosinase. Additionally, it demonstrates inhibitory activity against α-glucosidase. This compound is valuable for research in pigmentation, skin disorders, and carbohydrate metabolism. -
PPO Inhibitor
2,3-Diaminopropionic acid hydrochloride acts as an inhibitor of polyphenol oxidase (PPO), an enzyme involved in the browning reaction of fruits and vegetables. This compound serves as a key precursor for the synthesis of antibiotics and the siderophore staphyloferrin B. Its ability to modulate PPO activity makes it valuable for research in enzymology and agriculture, particularly in studies aimed at controlling oxidative processes in various biological systems.

