Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
(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. -
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. -
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. -
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. -
IDH Inhibitor
(S,S)-GSK321 is a selective inhibitor of isocitrate dehydrogenase (IDH), specifically targeting mutated forms of the enzyme. This compound exhibits significant anti-cancer activity by disrupting the metabolic pathways in cells with IDH mutations. It is primarily utilized in research focused on cancer therapeutics and metabolic disease modeling. -
IDH Inhibitor
Lanisidenib is an isocitrate dehydrogenase (IDH) inhibitor that displays potent antineoplastic activity. By targeting abnormal IDH enzymes, it disrupts metabolic pathways involved in tumor growth and survival. This compound is applicable in research focused on cancer metabolism and therapeutic strategies for IDH-mutated malignancies. -
IDH1 Inhibitor
IDH1 Inhibitor 5 is an inhibitor of isocitrate dehydrogenase 1 (IDH1), targeting both wild-type and mutant forms of the enzyme. It demonstrates potent biological activity with IC50 values of 64.4 nM in MOG cells and 34.9 nM in glioma cells expressing the exogenous mutant IDH1 R132H protein. This compound is valuable for research applications focused on glioma and other IDH1-related oncogenic processes. -
IDH2 R140Q Mutant Inhibitor
IDH2R140Q-IN-2 is a selective inhibitor targeting the IDH2 R140Q mutant with an IC50 of 29 nM. This compound effectively reduces the production of D2HG in TF-1 cell lines expressing the mutant IDH2 R140Q, demonstrating an IC50 of 10 nM. IDH2R140Q-IN-2 is useful for studying the role of mutant IDH2 in acute myeloid leukemia (AML) and can significantly suppress D2HG levels in tumor tissue. -
IDH2R140Q Inhibitor
IDH2R140Q-IN-1 is a selective inhibitor of the IDH2R140Q mutant isoform, demonstrating a potent inhibitory effect with an IC50 of 6.1 nM. This compound is primarily utilized in research focused on acute myeloid leukemia, contributing to the understanding of IDH2-driven oncogenesis and potential therapeutic strategies. Its application in preclinical studies may facilitate the development of targeted treatments aimed at malignancies associated with IDH mutations. -
IDH1-mutant Inhibitor
IHMT-IDH1-053 is a highly selective and irreversible inhibitor of IDH1 R132H mutants, with an IC50 of 4.7 nM. It demonstrates pronounced selectivity against IDH1 wild-type and various IDH2 isoforms. IHMT-IDH1-053 effectively inhibits the production of 2-hydroxyglutarate (2-HG) in IDH1 R132H mutant transfected 293T cells, achieving an IC50 of 28 nM. Additionally, this compound blocks the proliferation of HT1080 cell lines and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutants, providing valuable insights for therapeutic target validation in IDH1-mutant driven malignancies. -
IDH2/R140Q Inhibitor
CP-17 is a selective inhibitor of the IDH2/R140Q mutation, demonstrating an IC50 of 40.75 nM. It exhibits over 55-fold selectivity against wild-type IDH2, effectively reducing D-2-HG levels in TF-1 cells harboring the IDH2/R140Q mutation. Additionally, CP-17 effectively reverses the cellular differentiation blockade associated with the R140Q mutation, making it a valuable tool for research in acute myeloid leukemia (AML). -
IDH2 Mutant Inhibitor
TQ05310 is an orally bioavailable inhibitor of IDH2 mutants, specifically targeting IDH2-R140Q (IC50=136.9 nM) and IDH2-R172K (IC50=37.9 nM). It effectively inhibits the enzymatic activity of these mutants, resulting in reduced levels of 2-hydroxyglutarate (2-HG) and promoting differentiation in affected cells. TQ05310 is valuable for research applications focused on acute myeloid leukemia. -
IDH1 R132H Inhibitor
ML309 is a potent and selective inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H) with an IC50 of 96 nM. It acts as a competitive inhibitor of α-ketoglutarate (α-KG), exhibiting a Ki value of 156 nM while demonstrating minimal inhibition of wild-type IDH1. In in vitro studies, ML309 effectively decreases the production of the oncometabolite 2-hydroxyglutarate (2-HG) in U87MG cells. This compound serves as a valuable chemical probe for investigating the role of mutant IDH1 in cancer progression and therapeutic response. -
GSK321 Negative Control
GSK990 is an inactive mutant isocitrate dehydrogenase 1 (IDH1) inhibitor that exhibits no significant inhibitory activity against either wild-type or mutant IDH1/IDH2 enzymes. This compound is primarily utilized as a negative control in research studies involving the active IDH1 inhibitor GSK321. GSK990 is particularly relevant for investigations focusing on acute myeloid leukemia, enabling researchers to validate the specificity and efficacy of IDH1-targeted treatments. -
Mutant IDH1 Inhibitor
MRK-A is a selective inhibitor of mutant IDH1, demonstrating a potent IC50 value of 5 nM. By effectively inhibiting the production of 2-hydroxyglutarate (2-HG), MRK-A exhibits significant anti-cancer activity specifically against brain tumors. This compound is suited for research applications aimed at understanding the role of mutant IDH1 in tumorigenesis and exploring therapeutic strategies for brain cancer treatment. -
mIDH1 Inhibitor
mIDH1-IN-1 is a selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1) and exhibits an IC50 of 961.5 nM. This compound effectively reduces intracellular 2-hydroxyglutarate (2-HG) levels in HT1080 cells, demonstrating an EC50 of 208.6 ± 8.0 nM. Additionally, mIDH1-IN-1 displays significant anti-proliferative effects in IDH1 mutant U-87 cells, with an IC50 of 41.8 nM. This antitumor agent is valuable for research on IDH1-mutated solid tumors. -
mIDH2 Inhibitor
SH1573 is an orally active inhibitor of mutant isocitrate dehydrogenase 2 (mIDH2). It exhibits a strong and selective inhibitory effect on the mIDH2 R140Q variant, with an IC50 value of 4.78 nmol/L, effectively reducing the production of the oncogenic metabolite 2-hydroxyglutarate (2-HG) in various biological contexts, including animal models, cell lines, and tumors. SH1573 is designed for research applications in acute myeloid leukemia (AML) to investigate potential therapeutic strategies targeting mIDH2 mutations. -
IDH1-R132H Inhibitor
BRD2879 is a selective inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1-R132H), exhibiting an IC50 of 0.05 µM against this target. This compound effectively reduces levels of (R)-2-hydroxyglutarate (R-2HG), a metabolite associated with IDH mutations in various cancers. BRD2879 is valuable for research investigating IDH-related tumorigenesis and therapeutic strategies in malignant conditions driven by this mutation. -
mIDH1 Inhibitor
AGI-14100 is a potent mIDH1 inhibitor, exhibiting an IC50 of 6 nM. This compound has been carefully optimized to ensure metabolic stability and oral bioavailability, while minimizing human pregnane X receptor (hPXR) activation. AGI-14100 serves as a valuable tool for investigating the role of mutant isocitrate dehydrogenase 1 (mIDH1) in various cancer types, particularly those with IDH1 mutations. Its development enhances the understanding of mIDH1 inhibitors and their therapeutic potential in oncology research.
