Catalog No.
Product Name
Application
Product Information
Citations
-
IDH1 inhibitor
DH1 Inhibitor 2 is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.- Derek Dang, .et al. , Cancer Cell, 2025, Jun 9;43(6):1159-1174 PMID: 40378837
-
IDH2 inhibitor
Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).- Mohammed NadimSardoiwala, .et al. , Materials Science and Engineering: C, 2021, Dec 24 PMID: 35527145
-
IDH1 Inhibitor
GSK321 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), showing IC50 values of 2.9, 3.8, 4.6, and 46 nM for the R132G, R132C, R132H, and wild-type IDH1 variants, respectively, with over 100-fold selectivity for IDH2. This compound effectively reduces intracellular levels of α-Hydroxyglutaric acid (2-HG), disrupts the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. GSK321 is valuable for research on acute myeloid leukemia (AML) and various other malignancies. -
IDH1-R132H Inhibitor
Alpha-Mangostin is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1-R132H), demonstrating a Ki of 2.85 μM. This dietary xanthone exhibits a diverse range of biological activities, including antioxidant, anti-inflammatory, antibacterial, and anticancer properties. It is valuable for research applications exploring metabolic pathways in cancer and the development of targeted therapies against IDH1-mutant tumors. -
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. -
Mutant IDH1 Inhibitor
Mutant IDH1-IN-3 is a selective allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), demonstrating an IC50 of 13 nM specifically for the R132H IDH1 variant. By inhibiting this enzyme, Mutant IDH1-IN-3 effectively reduces the production of D-2-hydroxyglutaric acid (2HG) in cellular models. This compound is particularly valuable in cancer research, providing insights into metabolic alterations and therapeutic strategies targeting IDH1 mutations. -
IDH Inhibitor
Crelosidenib (gentisate) is a selective oral inhibitor of mutant isocitrate dehydrogenase (IDH) enzymes, specifically targeting IDH1 R132H (IC50 of 6.27 nM), IDH1 R132C (IC50 of 3.71 nM), IDH2 R140Q (IC50 of 36.9 nM), and IDH2 R172K (IC50 of 11.5 nM). It demonstrates decreased activity against wild-type IDH enzymes. Crelosidenib is primarily utilized in research focusing on metabolic dysregulation and oncogenic pathways associated with IDH mutations in various cancers. -
IDH1/2 Modulator
AGI-12026 is a brain-penetrant dual inhibitor targeting mutant isocitrate dehydrogenase 1 and 2 (IDH1/2). It acts as an allosteric modulator, demonstrating partial inhibition of the IDH1-R132H homodimer. This compound is suitable for research applications related to glioma and provides a valuable tool for studying the role of mutant IDH enzymes in cancer biology. -
IDHP Isomer
(R)-IDHP is an isomer of isovaleryl-DL-3-hydroxybutyric acid, functioning primarily by inhibiting Ca2+ release and modulating Ca2+ inward flow in both voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. This compound exhibits vasorelaxant properties and is valuable in research focused on cardiovascular disease mechanisms and treatments. Its biological activity makes it a useful tool for investigating vascular dynamics and related pathophysiological conditions. -
IDH1 inhibitor
AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity. -
IDH1 inhibitor
AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. -
mIDH1 inhibitor
BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). -
IDH1 Inhibitor
Vorasidenib, also known as AG-881, is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity. -
mutant IDH1 R132H inhibitor
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM. -
IDH inhibitor
Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay. -
mutant-selective IDH1 inhibitor
Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively. -
IDH1 inhibitor
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity. -
IDH1 inhibitor
Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia. -
IDH1 inhibitor
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ?? 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells. -
IDH1 inhibitor
IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H. -
IDH1 Inhibitor
IDH1 Inhibitor 9 is a selective inhibitor targeting isocitrate dehydrogenase 1 (IDH1), exhibiting IC50 values of 124.4 nM and 95.7 nM for the R132H and R132C mutations, respectively. This compound effectively induces apoptosis and promotes cell cycle arrest at the S phase. Due to its anti-tumor properties, IDH1 Inhibitor 9 is valuable for research in cancer biology and the development of targeted therapies in IDH1-mutated cancers.
