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Items 1751-1800 of 2992

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  1. Xanthine Oxidase Inhibitor

    (+/-)-Epicatechin is a xanthine oxidase inhibitor with an IC50 value of 982.14 μM. This compound, found in Semen Plantaginis (Plantago seed), showcases potential in research related to hyperuricemia and gout. Its ability to modulate xanthine oxidase activity makes it a valuable tool for investigating mechanisms underlying uric acid metabolism and associated pathologies.
  2. XO Inhibitor

    Tetrahydroamentoflavone is a potent xanthine oxidase (XO) inhibitor, demonstrating significant inhibitory activity with IC50 and Ki values of 92 nM and 0.982 μM, respectively. This compound has potential applications in the study of inflammatory disorders and gout, making it a valuable tool for researchers investigating these conditions. Its ability to modulate XO activity positions it as a promising candidate for further exploration in therapeutic contexts.
  3. XOD Inhibitor

    Xanthine oxidase-IN-9 is a selective inhibitor of xanthine oxidase (XOD), exhibiting an IC50 value of 31.81 μM. This compound is instrumental in studying disorders associated with increased XOD activity, including gout and oxidative stress-related conditions. Its biological activity makes it a valuable tool in biochemical research aimed at developing therapeutic strategies targeting purine metabolism and reactive oxygen species.
  4. Xanthine Oxidase Inhibitor

    Prudomestin is a potent xanthine oxidase inhibitor derived from the heartwood of Prunus domestica. With an IC50 of approximately 6 µM, it exhibits significant inhibitory activity against XO, a key enzyme involved in purine metabolism and the production of reactive oxygen species. This compound is valuable for research applications focused on oxidative stress, gout, and related inflammatory conditions.
  5. Xanthine Oxidase Inhibitor

    Xanthine oxidase-IN-4 is a potent inhibitor of xanthine oxidase (XO), exhibiting an IC50 of 0.039 μM. This compound demonstrates significant hypouricemic activity in potassium oxonate-induced models of hyperuricemia, making it suitable for investigations related to hyperuricemia and gout. Xanthine oxidase-IN-4 is valuable for researchers studying metabolic disorders and the pharmacological management of gout.
  6. Xanthine Oxidase Inhibitor

    Protosappanin A dimethyl acetal is a homoisoflavonoid that acts as a competitive inhibitor of xanthine oxidase. This compound demonstrates significant xanthine oxidase inhibitory activity, with an IC50 value of 50.7 μM. It is isolated from the plant species Caesalpinia sappan and is applicable in research focused on oxidative stress and related metabolic disorders.
  7. Xanthine oxidase Inhibitor

    Xanthine oxidase-IN-15 is a selective inhibitor of xanthine oxidase (XO) with an IC50 of 0.13 μM. This compound functions by forming a stable interaction at the active site of XO, effectively inhibiting its catalytic activity. Xanthine oxidase-IN-15 is primarily utilized in research related to hyperuricemia and gout, offering insights into the management and treatment of these conditions.
  8. Xanthine Oxidase Inhibitor

    Renierol is an orally active inhibitor of xanthine oxidase (XO), a critical enzyme involved in purine metabolism. It exhibits notable urate-lowering activity, making it valuable for research related to gout and hyperuricemia. This compound is essential for studying the role of XO in oxidative stress and related pathologies.
  9. Xanthine Oxidase Inhibitor

    5-Hydroxy-3,4,7-triphenyl-2,6-benzofurandione is a potent inhibitor of xanthine oxidase, an enzyme involved in the oxidative metabolism of purines. This compound exhibits significant biological activity in the reduction of uric acid levels, making it relevant for studies related to hyperuricemia and gout. Research applications include investigations into the mechanistic pathways of oxidative stress and potential therapeutic interventions for related disorders.
  10. XO Inhibitor

    BOF-4272 is a selective inhibitor of xanthine oxidase and xanthine dehydrogenase. This compound is primarily utilized in research focused on hyperuricemia and related disorders. By inhibiting uric acid production, BOF-4272 serves as a valuable tool for studying gout and other conditions associated with elevated uric acid levels.
  11. Xanthosine oxidase Inhibitor

    Hydroxyakalone is a potent inhibitor of xanthosine oxidase (XOD, EC 1.2.3.2), exhibiting an IC50 value of 4.6 μM. This compound is useful in research applications focused on oxidative stress and related metabolic pathways. Its ability to inhibit XOD may provide insights into the management of conditions associated with elevated levels of xanthine and uric acid.
  12. Xanthine Oxidase Inhibitor

    Xanthine oxidase-IN-14 is a potent inhibitor of xanthine oxidase, demonstrating an IC50 value greater than 100 μM. This compound has shown significant anti-proliferative activity against cancer cell lines, including MCF-7, NCI-H460, and SF-268, with inhibition occurring at an IC50 greater than 150 μM. It serves as a valuable tool for exploring the role of xanthine oxidase in cancer biology and potential therapeutic applications.
  13. Xanthine Oxidase Inhibitor

    Xanthine oxidase-IN-22 is a potent inhibitor of xanthine oxidase (XO) with an IC50 of 0.0034 μM, demonstrating a mixed-type inhibition profile. This compound effectively lowers serum uric acid levels in murine models. Xanthine oxidase-IN-22 is suitable for research applications focused on hyperuricemia and gout management.
  14. Xanthine Oxidase Inhibitor

    Xanthine oxidase-IN-1 is a potent inhibitor of xanthine oxidase, demonstrating an IC50 of 6.5 nM. This compound is valuable for research applications focusing on the modulation of purine metabolism and the investigation of conditions associated with oxidative stress, such as gout and cardiovascular diseases. Its ability to effectively inhibit xanthine oxidase makes it a useful tool in exploring therapeutic strategies for these disorders.
  15. β-Glucuronidase Inhibitor

    Saccharic acid is a competitive inhibitor of β-glucuronidase, a key enzyme involved in the hydrolysis of glucuronides. This compound effectively slows the hydrolysis of l-ortho-hydroxyphenylazo-2-naphthol glucuronide in frozen mouse kidney sections, making it a valuable tool for studying glucuronidation processes. While it demonstrates utility in renal studies, it does not influence liver regeneration following injury or growth in infant mice, ensuring specific applications in biochemical research.
  16. β-glucuronidase Inhibitor

    Ganoderenic acid A is a lanostane-type triterpene that functions as a potent inhibitor of β-glucuronidase. This compound demonstrates significant hepatoprotective properties, particularly in mitigating liver injury induced by carbon tetrachloride (CCl4). Ganoderenic acid A is valuable for research into liver disease mechanisms and the development of protective strategies against hepatotoxicity.
  17. β-glucuronidase Inhibitor

    4'',5''-Dehydroisopsoralidin is a potent inhibitor of β-glucuronidase, with an IC50 value of 6.3 μM. This compound exhibits significant anti-inflammatory and antioxidant properties, making it a valuable tool for research focused on inflammation and various cancer pathways. Its inhibition of β-glucuronidase can help elucidate the mechanisms underlying these biological processes.
  18. β-glucuronidase Inhibitor

    β-Glucuronidase-IN-4 is a non-competitive inhibitor of β-glucuronidase, exhibiting an IC50 of 2.68 μM and a Ki value of 1.64 μM. This compound has demonstrated potential in alleviating gastrointestinal adverse events associated with Escherichia coli infections by effectively inhibiting the activity of E. coli β-glucuronidase. Its application is relevant for research focused on gut microbiome interactions and microbial enzyme inhibition.
  19. MAO-B Inhibitor

    MAO-B-IN-9 is a selective, irreversible inhibitor of monoamine oxidase B (MAO-B) that effectively penetrates the blood-brain barrier, exhibiting an IC50 of 0.18 μM. This compound demonstrates neuroprotective effects by preventing Aβ1-42-induced neuronal cell death, potentially through its ability to inhibit Aβ1-42 aggregation. Additionally, MAO-B-IN-9 serves as a click chemistry reagent, featuring an alkyne group that readily participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions for versatile applications in chemical biology research.
  20. NMT Inhibitor

    Zelenirstat is a potent dual inhibitor of N-myristoyltransferase (NMT), exhibiting IC50 values of 5 nM for NMT1 and 8 nM for NMT2. This orally active small molecule induces apoptosis in cancer cells and demonstrates anti-cancer activity by inhibiting early B cell receptor (BCR) signaling. Zelenirstat is a valuable tool for investigating the mechanisms underlying malignant lymphoma and other related malignancies.
  21. N-myristoyltransferase Inhibitor

    LY134046 is an inhibitor of N-myristoyltransferase (NMT), primarily targeting norepinephrine N-methyltransferase in cardiovascular research. This compound produces sustained reductions in mean arterial blood pressure and heart rate without significantly altering norepinephrine concentrations in the rat brain. Notably, LY134046 does not engage with adrenergic or cholinergic receptors, indicating that its hypotensive and bradycardic effects operate independently of neurogenic tension. At a dosage of 40 mg/kg/day, LY134046 leads to significant inhibition of NMT activity in the hypothalamus and brainstem, thereby inducing central norepinephrine depletion.
  22. NMT Inhibitor

    NMT-IN-8 is a potent and selective inhibitor of N-myristoyl transferase (NMT), exhibiting an IC50 value of less than 10 nM. It effectively disrupts the catalyzed protein N-myristoylation by binding to the peptide binding pocket of NMT, thereby influencing critical biological pathways including protein trafficking, signal transduction, and viral replication. This compound is particularly relevant for research applications in oncology, such as MYC-addicted cancers and B-cell lymphoma, as well as in the study of infectious diseases, including malaria, HIV, and rhinovirus infections.
  23. NAMPT Inhibitor

    Nampt-IN-10 TFA is a potent inhibitor of Nicotinamide Phosphoribosyltransferase (NAMPT). It exhibits significant cellular potency against A2780 and CORL23 cell lines, with IC50 values of 5 nM and 19 nM, respectively. This compound serves as a promising non-antimitotic payload for antibody-drug conjugates (ADCs) in cancer research, highlighting its potential in therapeutic applications targeting NAMPT-related metabolic pathways.
  24. Nampt Inhibitor

    Nampt-IN-15 is an inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis through the inhibition of nicotinamide phosphoribosyltransferase (Nampt). It exhibits potent cytotoxicity in various cancer cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13, with IC50 values of 38.5 nM, 8 nM, 8.5 nM, and 7 nM, respectively. This compound is valuable for research applications focused on cancer metabolism and therapeutic strategies targeting NAMPT in tumor cells.
  25. NAMPT Inhibitor

    GNE-618 is a potent inhibitor of nicotinamide phosphoribosyl transferase (NAMPT) with an IC50 of 6 nM. By depleting cellular NAD levels, GNE-618 induces apoptosis in tumor cells, exhibiting significant anti-tumor activity. This compound is primarily applied in cancer research, facilitating the study of NAD metabolism and its implications in oncology.
  26. NAMPT Inhibitor

    GNE-617 hydrochloride is a potent inhibitor of NAMPT (Nicotinamide adenine dinucleotide biosynthesis regulator) with an IC50 of 5 nM. This compound effectively disrupts NAMPT enzymatic activity, leading to decreased levels of NAD+ in cellular systems. GNE-617 has demonstrated significant efficacy in various xenograft cancer models, making it a valuable tool for investigating cancer metabolism and the therapeutic potential of targeting NAD+ synthesis.
  27. NAMPT Inhibitor

    A-1293201 is a potent NAMPT inhibitor that demonstrates antitumor activity by reducing total cellular NAD+/NADH levels. This reduction leads to significant ATP depletion, ultimately resulting in the induction of cancer cell death. Additionally, A-1293201 effectively addresses the acquired resistance mechanism associated with the NAMPT Y18 mutant, providing a promising avenue for research in cancer treatment.
  28. NAMPT Inhibitor

    LB-60-OF61 hydrochloride is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), demonstrating significant cytotoxic effects. This compound shows selective activity against MYC-overexpressing cell lines, making it a valuable tool in cancer research. Its specific targeting of NAMPT allows for investigations into pathways related to cellular metabolism and cancer cell survival.
  29. NAMPT Inhibitor

    Nampt-IN-9 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis via the enzyme NAMPT. It exhibits significant anticancer activity and has potential applications in research focusing on pancreatic ductal adenocarcinoma. This compound serves as a valuable tool for studying the metabolic pathways and therapeutic strategies related to cancer treatment.
  30. NAMPT Inhibitor

    Nampt-IN-13 is a selective inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis through the inhibition of nicotinamide phosphoribosyltransferase (NAMPT). This compound demonstrates significant anti-proliferative effects and is utilized in the study of tumor metabolism and cancer therapy. Its application is particularly relevant in the synthesis of antibody-drug conjugates (ADCs) for targeted cancer treatment research.
  31. MS7

    NAMPT Inhibitor

    MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), which is often overexpressed in cancer cells to sustain NAD+ levels necessary for rapid cell proliferation. By targeting NAMPT, MS7 serves as a valuable tool for developing PROTAC A7, an effective degrader of NAMPT. This reagent holds significant potential for research applications in cancer biology, particularly in studies focused on metabolic regulation and therapeutic strategies targeting NAMPT.
  32. NAMPT Inhibitor

    Nampt-IN-7 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis by targeting NAMPT, with an IC50 of 7.31 μM. This compound exhibits significant cytotoxicity against the HepG2 hepatocellular carcinoma cell line, demonstrated by an IC50 of 24.28 μM. Nampt-IN-7 is valuable for research applications focusing on cancer metabolism and therapeutic strategies targeting NAD+ synthesis in tumor cells.
  33. NAMPT Inhibitor

    AS1604498 is a selective competitive inhibitor of human nicotinamide adenine dinucleotide (NAD) biosynthesis enzyme NAMPT, demonstrating an IC50 of 44.4 nM. By inhibiting NAMPT activity, AS1604498 effectively reduces the production of nicotinamide mononucleotide and lowers intracellular NAD levels, leading to the activation of caspase 3/7 and the subsequent induction of apoptosis in cancer cells. This compound is particularly relevant for research focused on chronic myeloid leukemia and related metabolic pathways.
  34. NAMPT Inhibitor

    Nampt-IN-17 is a selective inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis, targeting NAMPT with an IC50 of 17 nM and a Ki of 25.9 nM in human cells. This compound effectively depletes intracellular NAD+ and ATP levels, leading to disrupted mitochondrial membrane potential and subsequently inhibiting cell proliferation, self-renewal, invasion, and migration. Additionally, Nampt-IN-17 induces cell cycle arrest and apoptosis, demonstrating potent selectivity against NAPRT-deficient gastric cancer cells. It serves as a valuable tool for studying the mechanisms underlying NAPRT-deficient gastric cancer.
  35. PAI-1 Inhibitor

    Aleplasinin is a selective inhibitor of SERPINE1 (PAI-1) with an IC50 of 655 nM. By inhibiting PAI-1, Aleplasinin activates the tissue-type plasminogen activator (tPA)/fibrinolysis cascade, facilitating the degradation of amyloid-β (Aβ) oligomers and monomers. This compound has demonstrated significant efficacy in reducing plasma and brain Aβ levels, improving memory function, and reversing cognitive impairment. Aleplasinin is a valuable tool for research focused on Alzheimer’s disease and related neurodegenerative disorders.
  36. Ser/Thr Protease Inhibitor

    ZK824859 hydrochloride is a selective inhibitor of urokinase plasminogen activator (uPA) with a potent IC50 of 79 nM. It also demonstrates varied inhibitory effects on tissue plasminogen activator (tPA) and plasmin, with respective IC50s of 1580 nM and 1330 nM. This compound is particularly relevant for research applications focusing on serine/threonine proteases and their roles in pathological processes, including fibrinolysis and tumor progression. Its oral bioavailability makes it a valuable tool for in vivo studies targeting uPA-mediated pathways.
  37. PAI-1 Inhibitor

    SK-216 is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), playing a crucial role in reducing metastasis in human osteosarcoma. It has demonstrated efficacy in inhibiting lung metastasis associated with this malignancy, making it a valuable compound for research focused on cancer metastasis and therapeutic interventions in osteosarcoma. This compound is suitable for studies exploring the mechanisms of tumor invasion and potential anti-metastatic strategies.
  38. PAI-1 Inhibitor

    CDE-096 is a potent inhibitor of Plasminogen Activator Inhibitor-1 (PAI-1), effectively preventing PAI-1 from inactivating tissue plasminogen activator (tPA) and urokinase plasminogen activator (uPA) with comparable potency (IC50 values of 30 nM and 25 nM, respectively). It demonstrates efficacy against glycosylated forms of PAI-1 and possesses inhibitory activity against PAI-1 derived from various species, including murine, rat, and porcine models, with IC50 values of 19 nM, 22 nM, and 18 nM, respectively. CDE-096 is valuable for research focused on fibrinolysis, thrombolysis, and related cardiovascular studies.
  39. PAI-1 Inhibitor

    Diaplasinin is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), exhibiting an IC50 of 295 nM. This compound demonstrates significant antithrombotic activity, making it valuable for research into coagulation disorders. Its ability to modulate PAI-1 levels may provide insights into therapeutic strategies for conditions associated with thrombosis and fibrinolysis.
  40. PAI-1 Inhibitor

    Toddalolactone is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), demonstrating an IC50 value of 37.31 μM. This compound, derived from Toddalia asiatica, plays a critical role in modulating fibrinolysis and is of significant interest in research related to thrombosis and cardiovascular diseases. Its ability to inhibit PAI-1 activity makes it a valuable tool for investigating pathways involved in clot formation and resolution.
  41. PAI-1 Inhibitor

    AZ3976 is a selective inhibitor of plasminogen activator inhibitor type 1 (PAI-1) that demonstrates an IC50 value of 26 μM in enzymatic chromogenic assays and 16 μM in plasma clot lysis assays. This compound enhances the latency transition of active PAI-1 by reversibly binding to latent PAI-1, thereby facilitating fibrinolysis. AZ3976 is ideal for research applications focused on thrombosis and fibrinolytic processes.
  42. urokinase plasminogen activator Inhibitor

    28-O-β-D-Glucopyranosyl pomolic acid is an inhibitor of urokinase plasminogen activator, with an IC50 value of 37.82 μM. This compound can effectively modulate the fibrinolytic pathway by hindering the activation of plasminogen, thereby impacting processes related to fibrin degradation and tissue remodeling. It is suitable for research in fields such as cancer biology, fibrosis, and vascular disorders, where regulation of the uPA system is of significant interest.
  43. Plasminogen Activation Inhibitor

    BT-114143 is a plasminogen activation inhibitor, exhibiting an IC50 of 8.42 μM. This compound is valuable in research focused on hemorrhagic diseases stemming from hyperfibrinolysis, including traumatic bleeding, severe menstrual bleeding, postpartum hemorrhage, and complications associated with hemophilia. Its targeted inhibition of plasminogen activation positions it as a potential therapeutic agent in the management of these conditions.
  44. PAI-1 Inhibitor

    XR 5118 hydrochloride is a selective inhibitor of plasminogen activator inhibitor 1 (PAI-1), with an IC50 value of 12 µM. By binding to PAI-1, XR 5118 hydrochloride effectively reduces plasma PAI-1 activity, promoting endogenous thrombolysis and inhibiting thrombus formation. This compound is valuable for research applications related to cancer and thrombotic disorders, providing insights into mechanisms of fibrinolysis and clot regulation.
  45. PCSK9 Inhibitor

    PCSK9-IN-34 is a small molecule inhibitor targeting proprotein convertase subtilisin/kexin type 9 (PCSK9). It plays a crucial role in regulating cholesterol levels by preventing PCSK9-mediated degradation of LDL receptors. This compound is valuable for research into cardiovascular conditions and cholesterol metabolism, particularly in the context of hyperlipidemia and atherosclerosis.
  46. PCSK9/IDLR/SREBP2 mRNA Inhibitor

    5-O-Methylembelin is a natural isocoumarin that functions as an inhibitor of PCSK9, the inducible degrader of the low-density lipoprotein receptor (IDLR), and SREBP2 mRNA expression. This compound is essential for studying lipid metabolism and cholesterol regulation, making it valuable for research focused on hypercholesterolemia and cardiovascular diseases. Its ability to modulate these crucial pathways enables exploration of potential therapeutic strategies targeting lipid homeostasis.
  47. PCSK9 Inhibitor

    PCSK9-IN-10 is a potent oral inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibiting an IC50 value of 6.4 µM. This compound enhances the expression of LDL receptors (LDLR) while downregulating PCSK9 levels, contributing to the reduction of atherosclerosis progression. PCSK9-IN-10 is suitable for research applications focused on hyperlipidemia and cardiovascular diseases.
  48. PCSK9 Inhibitor

    PCSK9-IN-11 is a potent, orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It demonstrates effective transcriptional inhibitory activity in HepG2 cells, with an IC50 value of 5.7 μM. By increasing the protein level of LDL receptors (LDLR), PCSK9-IN-11 serves as a valuable tool for research in atherosclerosis and lipid metabolism.
  49. PCSK9 inhibitor

    PCSK9-IN-23 is a potent inhibitor of PCSK9, effectively blocking its secretion from HepG2 cells. This inhibition leads to a significant increase in LDL receptor (LDLR) expression, making it valuable for research aimed at understanding lipid metabolism and developing therapeutic strategies for hyperlipidemia and cardiovascular diseases. Its ability to modulate LDLR provides insights into cholesterol regulation and potential interventions in related disorders.
  50. PCSK9 Inhibitor

    PCSK9-IN-13 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), significantly disrupting its interaction with low-density lipoprotein (LDL) receptors. With an IC50 value of 537 nM, this compound is instrumental in studying lipid metabolism and cardiovascular diseases. Its application in research can facilitate the development of novel therapeutics for disorders associated with dyslipidemia.

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