Metabolism

Items 3751-3800 of 6168

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  1. IDO1 Inhibitor

    (S)-LY-3381916 is a selective inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1), demonstrating potent activity with an IC50 value of less than 1.5 µM. This S-isomer effectively binds to the apo-IDO1 form, targeting the enzyme in its unbound state and circumventing the heme-bound variant. Research applications include investigating the role of IDO1 in immunoregulation and exploring therapeutic strategies in cancer and inflammatory diseases.
  2. IDO1 Inhibitor

    (Rac)-LY-3381916 is a potent inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1), specifically targeting its apo- form. This racemic compound demonstrates selective inhibition of IDO1 activity and is capable of penetrating the blood-brain barrier. Its unique mechanism of action makes it valuable for research applications focused on immunotherapy and neurological diseases where modulation of the kynurenine pathway is critical.
  3. IDO1 Inhibitor

    IDO-IN-8 is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with an IC50 range of 1-10 μM. This compound is derived from patent WO2012142237A1 and is utilized in research to elucidate the role of IDO1 in immune regulation and tumor microenvironments. IDO-IN-8 is particularly relevant in studies focused on cancer immunotherapy and the modulation of immune responses.
  4. IDO1 PROTAC Degrader

    NU227326 is a potent IDO1 PROTAC degrader designed to penetrate the blood-brain barrier, exhibiting a DC50 of 4.5 nM in HiBiT degradation assays. It effectively degrades IDO1 in human glioblastoma cell lines U87 and GBM43, with DC50 values of 7.1 nM and 11.8 nM, respectively, as demonstrated in Western blot assays. This compound is valuable for research into various malignancies, including glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer.
  5. IDO1 Inhibitor

    BMT-297376 is a potent inhibitor of Indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme implicated in the modulation of immune responses and tumor microenvironments. This compound has shown significant biological activity by effectively blocking IDO1, which can enhance anti-tumor immunity and alleviate immune evasion in various cancer models. BMT-297376 is a valuable tool for researchers investigating immune modulation and the therapeutic potential of IDO1 inhibition in oncology.
  6. PROTAC IDO1 Degrader

    NU223612 is a selective PROTAC designed to target and degrade indoleamine 2,3-dioxygenase 1 (IDO1) through CRBN-mediated proteasomal degradation, exhibiting a Kd of 640 nM. With a binding affinity for CRBN of 290 nM, NU223612 effectively reduces IDO1 protein levels, making it a valuable tool in the study of immune modulation and tumor microenvironments. Additionally, NU223612 demonstrates the ability to cross the blood-brain barrier, enhancing its potential utility in neurobiological research.
  7. IDO1 Inhibitor

    IDO-IN-6 (NLG-1486) is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO1), demonstrating an IC50 of less than 1 μM. This compound plays a critical role in modulating immune responses by inhibiting tryptophan catabolism, making it a valuable tool in cancer immunotherapy and research on immune regulation. IDO-IN-6 is extensively utilized in studies investigating tumor microenvironments and the effects of IDO1 inhibition on immune system activity.
  8. IDO Inhibitor

    IDO1-IN-11 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 value of 0.6 nM. This compound exhibits significant activity in modulating immune responses by inhibiting tryptophan catabolism, thereby enhancing T cell function. IDO1-IN-11 is valuable for research applications investigating cancer immunotherapy and immune regulation.
  9. IDO1 Inhibitor

    IDO1-IN-7 is a potent and selective inhibitor of indoleamine-2,3-dioxygenase-1 (IDO1), exhibiting an IC50 of 6.1 nM in cellular assays using SKOV3 cancer cells. This compound modulates immune responses, making it a valuable tool for investigating immunotherapeutic strategies in cancer research. IDO1-IN-7 is suitable for studies aimed at understanding the role of IDO1 in tumor immune evasion and identifying potential therapeutic interventions.
  10. IDO1/IDO2 Inhibitor

    IDO1/2-IN-1 hydrochloride is a potent dual inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) and indoleamine 2,3-dioxygenase 2 (IDO2), with IC50 values of 28 nM and 144 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its oral bioavailability facilitates its use in various biological studies aimed at understanding immune modulation and tumor microenvironment interactions.
  11. IDO1 Inhibitor

    NUCC-0223619 is an IDO1 inhibitor that induces degradation of the indoleamine 2,3-dioxygenase 1 (IDO1) protein. This compound serves as a valuable tool for studying the immunomodulatory effects of IDO1 inhibition and is applicable in further research, including the synthesis of PROTACs (PROteolysis TArgeting Chimeras). Researchers can utilize NUCC-0223619 to investigate its potential impact on tumor microenvironments and immune responses.
  12. IDO1 Inhibitor

    IDO1-IN-17 is a selective inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 0.44 μM in HeLa cells. By blocking IDO1, this compound modulates the kynurenine pathway and impairs tryptophan catabolism, leading to enhanced immune response. IDO1-IN-17 is a valuable tool for research into cancer immunotherapy and the exploration of immune metabolism.
  13. IDO1/TDO Inhibitor

    IDO1/TDO-IN-3 is a potent inhibitor targeting both indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO). It demonstrates significant inhibitory potency with IC50 values of 0.005 μM for IDO1 and 0.004 μM for TDO. This compound exhibits considerable anti-tumor activity in vivo while displaying no apparent toxicity, making it a valuable tool for studies in cancer immunotherapy and metabolism.
  14. IDO Inhibitor

    IDO-IN-15 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with an IC50 value of less than 0.51 nM. This compound is utilized in research focused on cancer immunity, neurodegenerative diseases, and inflammation due to its ability to modulate the immune response by inhibiting tryptophan catabolism. Its high specificity and efficacy make it a valuable tool for investigating the therapeutic potential of targeting IDO1 in various biological contexts.
  15. IDO1 Inhibitor

    MMG-0358 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 2 nM in cellular assays against murine IDO1 (mIDO1) and 80 nM against human IDO1 (hIDO1). Additionally, it displays IC50 values of 330 nM and 71 nM in enzymatic assays of hIDO1 at pH 6.5 and pH 7.4, respectively. This compound is a valuable tool for studying immune regulation and may have applications in cancer immunotherapy and related research fields.
  16. IDO1/TDO Inhibitor

    IDO1/TDO-IN-8 is a dual inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1) and tryptophan-2,3-dioxygenase (TDO) with the ability to penetrate the blood-brain barrier. It exhibits EC50 values of 0.33 μM for IDO1 and 1.78 μM for TDO, effectively reducing the kynurenine/tryptophan ratio by modulating the kynurenine pathway of tryptophan metabolism. This compound demonstrates neuroprotective properties, alleviating motor dysfunction and mitigating depressive symptoms, making it a valuable tool in the investigation of neurodegenerative disorders such as Parkinson's disease co-occurring with depression.
  17. IDO Inhibitor

    CAY10581 is a pyranonaphthoquinone derivative that functions as a highly specific and reversible uncompetitive inhibitor of indoleamine 2,3-dioxygenase (IDO). With an IC50 value of 55 nM, this compound effectively blocks IDO-mediated tryptophan catabolism. CAY10581 is valuable for research in cancer immunotherapy and studies of immune modulation, providing insights into the role of IDO in various pathological conditions.
  18. IDO1/TDO2 Dual Inhibitor

    IDO1-IN-25 is a dual inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2), exhibiting IC50 values of 0.17 μM and 3.2 μM, respectively. This compound demonstrates the ability to effectively inhibit nitric oxide production in LPS-stimulated RAW264.7 cells, highlighting its anti-inflammatory potential. Additionally, IDO1-IN-25 has been shown to reduce inflammation in a mouse ear edema model induced by croton oil, making it a valuable tool for studying inflammatory pathways and immune responses.
  19. Apo-IDO1 Inhibitor

    IDO1-IN-29 is a selective inhibitor of apo-IDO1, exhibiting an IC50 of 0.29 μM. This compound effectively disrupts heme binding, making it a valuable tool for investigating the role of IDO1 in cancer biology. IDO1-IN-29 is particularly useful for researchers studying tumor immune evasion and exploring novel therapeutic strategies in oncology.
  20. IDO Antagonist

    IDO Antagonist-1 is a selective inhibitor of indoleamine 2,3-dioxygenase (IDO), a key enzyme involved in tryptophan catabolism and immune modulation. This compound effectively inhibits the growth of pancreatic adenocarcinoma cells in C57BL/6 mouse models, highlighting its potential utility in cancer research and immunotherapy. Researchers exploring the role of immune evasion in tumors may find this reagent essential for advancing therapeutic strategies.
  21. IDO1 Inhibitor

    IDO1-IN-23 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), displaying an IC50 value of 13 μM. This compound exhibits strong biological activity in modulating immune responses by inhibiting the enzymatic activity of IDO1, which is crucial for tryptophan degradation. IDO1-IN-23 is valuable for research applications focusing on immunotherapy and the tumor microenvironment, offering insights into immune evasion mechanisms in various cancers.
  22. IDO1 Inhibitor

    Roxyl-9 is an inhibitor of Indoleamine 2,3-dioxygenase 1 (IDO1), a key enzyme in the kynurenine pathway that regulates immune responses. This compound demonstrates significant biological activity by modulating tryptophan metabolism and can enhance anti-tumor immunity, making it a valuable tool in cancer research. Roxyl-9 is useful in studies aimed at understanding immune evasion mechanisms and developing therapeutic strategies targeting IDO1.
  23. IDO1/TDO Inhibitor

    IDO1/TDO-IN-2 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) with IC50 values of 0.1 μM and 0.07 μM, respectively. This compound demonstrates significant inhibitory effects that may be beneficial in cancer research, particularly in studies exploring immune modulation and tumor microenvironment interactions. Researchers can utilize IDO1/TDO-IN-2 to investigate therapeutic strategies targeting immunosuppression in cancer.
  24. IDO Inhibitor

    IDO-IN-16 is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO), demonstrating an IC50 of 36 nM. This compound effectively modulates the kynurenine pathway, leading to enhanced immune responses. IDO-IN-16 is applicable in cancer research, immunology, and studies aimed at understanding immune tolerance mechanisms.
  25. NAMPT/IDO1 Inhibitor

    NAMPT/IDO1-IN-1 is a dual inhibitor of NAMPT and IDO1, exhibiting IC50 values of 57.7 nM and 233 nM, respectively. By inhibiting NAMPT, this compound interferes with NAD+ biosynthesis, thereby suppressing the proliferation and migration of drug-resistant NSCLC cell lines, such as A549/R. Additionally, NAMPT/IDO1-IN-1 demonstrates significant antitumor activity in vivo and enhances the sensitivity of these resistant cells to paclitaxel treatment. This compound is valuable for research in cancer biology and the development of therapeutic strategies aimed at overcoming drug resistance.
  26. IDO Peptide

    Imsamotide, also known as IDO194-214, is an Indoleamine 2,3-Dioxygenase (IDO) peptide with the sequence DTLLKALLEIASCLEKALQVF. This compound serves as an immunological agent for active immunization, contributing to the modulation of immune responses. Additionally, Imsamotide exhibits potential antineoplastic properties, making it a valuable tool in cancer research and immunotherapy applications.
  27. IDO Inhibitor

    IDO1-IN-20 is an inhibitor of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme, which catalyzes the oxidative metabolism of tryptophan. This compound exhibits significant immunosuppressive effects within the tumor microenvironment, making it a valuable tool for cancer research. Its inhibition of IDO1 has potential applications in enhancing anti-tumor immune responses and studying the role of tryptophan metabolism in cancer progression.
  28. IDO1 Inhibitor

    IDO1-IN-21 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 value of 0.64 μM. This compound demonstrates significant anti-tumor activity, effectively inhibiting tumor growth in murine models. IDO1-IN-21 is valuable for research applications focused on cancer immunotherapy and the modulation of tryptophan metabolism in tumors.
  29. IDO1 Inhibitor

    1-Isopropyltryptophan is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1). It effectively reduces the expression of interferon-gamma stimulated IDO1 and IDO2 mRNA, thereby modulating immune responses. This compound is valuable for research focusing on cancer immunotherapy and the modulation of immune tolerance.
  30. IDO1 Inhibitor

    IDO1-IN-15 is a potent inhibitor of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme, with an IC50 value of 127 nM. This compound demonstrates comparable efficacy against IDO1 in vitro, making it a valuable tool for researchers investigating immune modulation and tumor microenvironments. IDO1-IN-15 is ideal for studies focused on cancer immunotherapy and related fields.
  31. IDO1 Inhibitor

    IDO1-IN-31 is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 of 77 nM. It is primarily utilized in research focused on neurological diseases and cancer. By modulating IDO1 activity, this compound contributes to studies investigating immune regulation and tumor microenvironment dynamics.
  32. IDO Inhibitor

    IDO1-IN-12 is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme involved in the catabolism of tryptophan and immune regulation. This compound exhibits significant efficacy in blocking IDO1 activity, thereby enhancing T-cell function and promoting anti-tumor immunity. IDO1-IN-12 is valuable for research applications focused on cancer immunotherapy and understanding immune escape mechanisms.
  33. IDO1 Inhibitor

    IDO1-IN-22 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with biochemical and cellular IC50 values of 67.4 nM and 17.6 nM, respectively, in human HeLa cells. This compound demonstrates significant antitumor activity in LLC xenograft models and possesses a favorable pharmacokinetic profile, making it a valuable tool for cancer research and therapeutic development targeting immune modulation pathways.
  34. Selective IDO1 Inhibitor

    IDO1-IN-2 is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting IC50 values of 81 nM in human, 59 nM in mouse, and 28 nM in rat models. This compound demonstrates significant anti-cancer activity, making it a valuable tool for exploring tumor immune evasion mechanisms. It is suitable for research applications focused on cancer immunotherapy and metabolism.
  35. IDO1 Inhibitor

    IDO1-IN-32 is a highly effective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an impressive IC50 of 10 pM. This compound demonstrates marked anti-proliferative effects in HeLa cells and has been shown to significantly inhibit tumor growth in CT26 and LCC models in vivo, primarily through the activation of anti-tumor immunity. IDO1-IN-32 is valuable for research exploring therapies in colon and breast cancer.
  36. IDO Inhibitor

    IDO-IN-14 is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO), exhibiting an IC50 value of 0.6928 nM. This compound effectively modulates tryptophan metabolism, a pathway crucial for immune regulation. IDO-IN-14 is primarily utilized in research focused on cancer immunotherapy and neurodegenerative disorders, where IDO activity is implicated in immune evasion and inflammation.
  37. IDO/TDO Inhibitor

    (R)-IDO/TDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor. It demonstrates notable anti-tumor activity in the MC38 xenograft model and exhibits synergistic effects when combined with anti-PD-1 monoclonal antibodies, such as SHR-1210. This compound is applicable in cancer research, particularly in studying immune modulation and therapeutic strategies targeting the kynurenine pathway.
  38. IDO1 Inhibitor

    IDO1-IN-16 is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), demonstrating an IC50 of 127 nM against the holoenzyme. This compound is essential for research applications in immunology, particularly in studying tumor microenvironments and modulating immune responses. IDO1-IN-16 can aid in the development of novel therapeutic strategies for cancer and autoimmune diseases by inhibiting the enzymatic activity that leads to immune tolerance.
  39. IDO Inhibitor

    IDO-IN-19 is a potent inhibitor of Indoleamine 2,3-Dioxygenase (IDO), an enzyme involved in the catabolism of tryptophan. By inhibiting IDO, this compound can restore T cell function, making it a valuable tool in the study of various conditions. Research applications include cancer immunotherapy, autoimmune disorders, infections, and neurodegenerative diseases like breast cancer and Alzheimer's disease.
  40. IDO1 Inhibitor

    IDO1-IN-26 is a selective inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1). This compound has demonstrated key biological activity in modulating immune responses and has potential applications in the study of sarcopenia and age-related muscle loss. Its ability to influence IDO1 activity makes it a valuable tool for researchers investigating metabolic and age-related conditions.
  41. IDO1 Inhbitor

    Linrodostat mesylate is a selective irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1). It exhibits potent biological activity, demonstrating an IC50 of 1.1 nM against IDO1-HEK293 cells. This compound plays a significant role in cancer research, particularly in the exploration of immune modulation and advanced cancer therapies.
  42. IDH1 Negative Control

    IDH1 ligand 1 serves as a negative control for isocitrate dehydrogenase 1 (IDH1). It exhibits no measurable affinity for wild-type IDH1, with an IC50 greater than 10,000 nM. This compound is useful in differentiating specific IDH1 interactions in research applications, allowing for the assessment of ligand-target relationships in biochemical assays.
  43. Aconitase/Isocitrate Dehydrogenase Inhibitor

    Oxalomalic acid trisodium is a potent inhibitor of aconitase and NADP-dependent isocitrate dehydrogenase. This compound demonstrates the ability to inhibit nitrite production and reduce iNOS protein expression in lipopolysaccharide-activated J774 macrophages. Oxalomalic acid trisodium is valuable for research focused on metabolic pathways and inflammatory responses.
  44. WT IDH1 Inhibitor

    (R,R)-GSK321 is a selective inhibitor of wild-type isocitrate dehydrogenase 1 (WT IDH1), exhibiting an IC50 value of 120 nM. This compound also shows inhibitory activity against the mutant R132H IDH1 variant, highlighting its potential in targeting IDH1-related metabolic pathways. It is useful for research applications focused on cancer metabolism and therapeutic development in tumors harboring IDH1 mutations.
  45. IDH1-mutant Inhibitor

    Safusidenib is a selective inhibitor targeting mutant isocitrate dehydrogenase 1 (IDH1), specifically effective against IDH1R132H and IDH1R132C variants. This compound demonstrates robust anticancer activity by impairing tumor growth in chondrosarcoma, exhibiting IC50 values of 15 nM and 130 nM, respectively. Safusidenib is of particular interest in studies focused on IDH1-mutant-associated malignancies, making it a valuable tool for cancer research and therapeutic exploration.
  46. IDH1 Inhibitor

    Crelosidenib is a selective inhibitor targeting mutant isocitrate dehydrogenase 1 (IDH1), demonstrating potent activity with IC50 values of 6.27 nM for IDH1 R132H and 3.71 nM for IDH1 R132C. Additionally, it shows inhibitory effects on IDH2 mutants, with IC50s of 36.9 nM for IDH2 R140Q and 11.5 nM for IDH2 R172K. Crelosidenib is primarily employed in research focused on IDH1 and IDH2 mutations, particularly in the context of cancer therapies.
  47. (S,R)-enantiomer of GSK321

    (S,R)-GSK321 is the (S,R)-enantiomer of GSK321, a selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It exhibits potent inhibitory activity with IC50 values of 2.9 nM for R132G, 3.8 nM for R132C, 4.6 nM for R132H, and 46 nM for wild-type IDH1, displaying over 100-fold selectivity for IDH1 compared to IDH2. This compound effectively reduces intracellular levels of 2-hydroxyglutarate (2-HG), alleviates the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. (S,R)-GSK321 is relevant for research into acute myeloid leukemia (AML) and related malignancies.
  48. IDH1 Inhibitor

    IDH1 Inhibitor 7 is a selective inhibitor of isocitrate dehydrogenase 1 (IDH1) with an IC50 of less than 100 nM. This compound is useful for studying the metabolic pathways involved in cancer, particularly in tumors with IDH1 mutations. It provides valuable insight into the role of IDH1 in cellular metabolism and offers potential applications in the development of targeted cancer therapies.
  49. Isocitrate Dehydrogenase Inhibitor

    Ranosidenib is an isocitrate dehydrogenase (IDH) inhibitor that exhibits significant antitumor activity. By targeting the IDH enzyme, it disrupts metabolic pathways critical for cancer cell proliferation. This compound is primarily utilized in research applications focused on cancer metabolism and therapeutic strategies for IDH-mutant tumors.
  50. IDH1 Inhibitor

    TC-E 5008 is a selective inhibitor of mutant IDH1, demonstrating potent activity with Ki values of 190 nM and 120 nM for the R132H and R132C mutants, respectively, while exhibiting minimal activity against wild-type IDH1 (Ki = 12.3 μM). This compound displays anti-proliferative effects on various estrogen receptor-positive breast cancer cell lines, making it a valuable tool for cancer research focusing on IDH1 mutations. TC-E 5008 is useful in exploring therapeutic strategies for cancers associated with these specific IDH1 mutations.

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