Metabolism

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  1. PPO Inhibitor

    PPO-IN-6 is a potent protoporphyrinogen oxidase (PPO) inhibitor that disrupts heme and chlorophyll biosynthesis. By inhibiting PPO activity, PPO-IN-6 can be utilized in cancer research and the investigation of other diseases linked to altered porphyrin metabolism. This compound serves as a valuable tool for studying the biochemical pathways involved in disease progression and therapeutic interventions.
  2. PPO Inhibitor

    PPO-IN-15 is a potent inhibitor of protoporphyrinogen IX oxidase (PPO), targeting a key enzyme in the biosynthesis of chlorophyll. This compound demonstrates effective herbicidal activity against resistant weed species, making it a valuable tool in agricultural research. Its selectivity profiles indicate reduced phytotoxicity, particularly in wheat and rice, enhancing crop safety while managing weed populations. This functionality makes PPO-IN-15 suitable for studies aimed at developing sustainable weed management strategies.
  3. PKM2 Kinase Inhibitor

    PKM2-IN-3 is a selective inhibitor of the PKM2 kinase, demonstrating an IC50 value of 4.1 μM. This compound exhibits notable anti-neuroinflammatory effects by disrupting PKM2-mediated glycolysis and inhibiting NLRP3 activation. PKM2-IN-3 is suitable for research applications focused on metabolic regulation and neuroinflammation pathways.
  4. PKM2 Inhibitor

    CIAC001 is a potent inhibitor of Pyruvate Kinase M2 (PKM2), demonstrating noteworthy anti-neuroinflammatory properties. It effectively suppresses LPS-induced nitric oxide (NO) production in BV-2 microglial cells, with an IC50 of 2.5 μM, and exhibits protective effects against neuroinflammation in various mouse models. Additionally, CIAC001 has shown the potential to inhibit aspects of chronic morphine-induced addiction, making it a valuable reagent for research into neuroinflammatory processes and addiction pathways.
  5. PKM2 Inhibitor

    NPD10084 is a potent inhibitor of pyruvate kinase M2 (PKM2) that targets non-glycolytic signaling in cancer cells. By disrupting the interaction between PKM2 and key regulatory proteins such as β-catenin and STAT3, NPD10084 effectively inhibits downstream signaling pathways. This compound exhibits significant antiproliferative activity against colorectal cancer cells, making it a valuable tool for cancer research and therapeutic investigations.
  6. MRSA Pyruvate Kinase Inhibitor

    Deoxytopsentin is a marine bisindole alkaloid that functions as an inhibitor of pyruvate kinase in methicillin-resistant Staphylococcus aureus (MRSA). This compound demonstrates significant antibacterial activity against MRSA strains in vitro. Deoxytopsentin is derived from sponges and serves as a valuable research tool for studying bacterial metabolism and developing therapies targeting antibiotic-resistant infections.
  7. AADC/PKM2 Inhibitor

    Benserazide is an inhibitor of aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase, primarily targeting the PKM2 enzyme. By binding directly to PKM2, Benserazide inhibits its activity, resulting in the suppression of aerobic glycolysis and the concurrent upregulation of oxidative phosphorylation (OXPHOS). This compound is valuable for research applications related to Parkinson's disease and melanoma.
  8. PKM2 Inhibitor

    PKM2-IN-4 is a selective inhibitor of pyruvate kinase M2 (PKM2), exhibiting an IC50 of 0.35 μM. This compound is known to regulate pyruvate-dependent respiration and promotes mitochondrial H2O2 production, impacting the efficiency of the electron transport system. It serves as a valuable tool in research focused on metabolism, cancer biology, and oxidative stress.
  9. PKM2 Inhibitor

    PKM2-IN-9 is a selective inhibitor of pyruvate kinase M2 (PKM2), achieving an inhibition rate of 75% at a concentration of 50 μM. This compound is of significant interest in cancer research, as it regulates metabolic pathways essential for tumor growth and survival. PKM2-IN-9 can be utilized to explore the role of PKM2 in cellular processes and as a potential therapeutic target in various types of cancer.
  10. Elk3 Inhibitor

    Alkannin is a selective inhibitor of tumor-specific pyruvate kinase-M2 (PKM2), demonstrating potent activity without affecting PKM1 or pyruvate kinase-L (PKL). This compound has potential applications in cancer research, serving as a valuable tool for studying metabolic alterations in tumors and developing anticancer strategies. Alkannin's specificity for PKM2 highlights its utility in targeted therapeutic approaches in oncology.
  11. Pyruvate Kinase Inhibitor

    PKM2-IN-5 is a selective inhibitor of pyruvate kinase M2 (PKM2), a critical enzyme involved in cellular energy metabolism. This compound exhibits potential for modulating glucose metabolism and influencing tumorigenesis by inhibiting PKM2 activity. PKM2-IN-5 is valuable for research applications in cancer biology and metabolic disorders, providing insights into the role of PKM2 in various cellular processes.
  12. Inverse RAR Inhibitor

    BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist that enhances nuclear corepressor interaction with RARs, effectively inhibiting retinoic acid-induced differentiation. This compound serves as a valuable tool in research applications focused on RAR signaling pathways and their regulatory mechanisms. Additionally, BMS493 features an alkyne group, enabling its use in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating diverse labeling and conjugation strategies.
  13. Nuclear Retinoic Acid Receptor γ Inhibitor

    BMS270394 is a selective inhibitor of the nuclear retinoic acid receptor gamma (RAR-γ), exhibiting an EC50 of 30 nM for human RAR-γ. This compound demonstrates potent activity against RAR-β with an EC50 of 400 nM. BMS270394 is valuable in research applications focused on gene regulation, developmental biology, and potential therapeutic interventions related to retinoid signaling pathways.
  14. RAR/RXR Inhibitor

    RXR Antagonist 5 is a selective retinoic acid X receptor (RXR) inhibitor, designed to modulate RXR activity. It effectively disrupts RXR signaling pathways, making it a valuable tool for investigating the role of RXR in various biological processes. This compound can be utilized in research applications focused on cancer biology, metabolism, and developmental studies, providing insights into RXR-mediated physiological functions.
  15. RAR/RXR Inhibitor

    NBD-125 is a potent RAR/RXR inhibitor that modulates retinoic acid receptor signaling. It functions as an RXRα activator, demonstrating an IC50 of 31.10 μM in KM12C cells. This compound is valuable for research applications involving the regulation of gene expression and signaling pathways associated with nuclear receptor activity.
  16. RAR/RXR Inhibitor

    AGN 191701 is a selective retinoic acid receptor (RAR) and retinoid X receptor (RXR) inhibitor. This compound has been shown to induce liver enlargement in rat models while preserving hepatocellular integrity, indicating a unique biological profile. AGN 191701 serves as a valuable tool for studying retinoid signaling pathways and their implications in hepatic processes.
  17. angiotensin-converting enzyme Inhibitor, renin Inhibitor

    Lyciumin D functions as both an angiotensin-converting enzyme inhibitor and a renin inhibitor. This compound demonstrates significant potential in the modulation of the renin-angiotensin system, making it a valuable tool for research into hypertension and related cardiovascular conditions. Its multimodal mechanism can facilitate studies aimed at understanding blood pressure regulation and developing therapeutic strategies for hypertension management.
  18. Serine Protease Inhibitor

    VD5123 is a potent serine protease inhibitor that effectively targets TMPRSS2, HGFA, matriptase, and hepsin, exhibiting IC50 values of 15 nM, 3980 nM, 140 nM, and 37 nM, respectively. This compound is particularly useful for antiviral research, including studies focused on SARS-CoV-2 and a broad spectrum of coronaviruses, as well as influenza viruses. Its ability to inhibit key proteases makes VD5123 an important tool in the investigation of viral pathogenesis and therapeutic development.
  19. Ser/Thr Protease Inhibitor

    Nacresertib is a selective Ser/Thr protease inhibitor that targets specific proteolytic pathways within cells. This compound is pivotal in studying cellular signaling mechanisms and apoptosis, making it valuable for research focused on cancer and neurodegenerative diseases. Its ability to modulate protease activity allows for the exploration of therapeutic strategies in various pathological states.
  20. Sex Pheromone Inhibitor

    iPD1 is a potent inhibitor of the sex pheromone cPD1, targeting pheromone signaling pathways. This compound effectively blocks the biological activity of sex pheromones, making it valuable in studies related to behavioral ecology and reproductive biology. Its application in research can provide insights into pheromone-mediated communication and its ecological impacts.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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