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Mutant IDH1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-104042
    Vorasidenib
    5+ Cited Publications

    AG-881

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
    Vorasidenib
  • HY-N0328
    alpha-Mangostin
    5+ Cited Publications

    α-Mangostin

    		 Reactive Oxygen Species (ROS) Apoptosis Bacterial Fungal Virus Protease Cancer
    alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
    alpha-Mangostin
  • HY-114226
    Olutasidenib
    3 Publications Verification

    FT-2102

    		 Isocitrate Dehydrogenase (IDH) Inflammation/Immunology Cancer
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
    Olutasidenib
  • HY-104036
    IDH-305
    4 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)) .
    IDH-305
  • HY-18082
    AGI-5198
    Maximum Cited Publications
    20 Publications Verification

    IDH-C35

    		 Isocitrate Dehydrogenase (IDH) Cancer
    AGI-5198 (IDH-C35) is a potent and selective mutant IDH1 R132H inhibitor with an IC50 of 0.07 μM.
    AGI-5198
  • HY-18948
    GSK321
    1 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. GSK321 induces decrease in intracellular α-Hydroxyglutaric acid (2-HG) (HY-113038B), abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
    GSK321
  • HY-12475
    Mutant IDH1-IN-1
    2 Publications Verification

    Agios 135

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1 R132H and IDH1 R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research .
    Mutant IDH1-IN-1
  • HY-100020
    BAY-1436032
    3 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
    BAY-1436032
  • HY-13972
    Mutant IDH1 inhibitor
    2 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
    Mutant IDH1 inhibitor
  • HY-129545
    DS-1001b
    2 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity .
    DS-1001b
  • HY-145594
    Safusidenib
    2 Publications Verification

    AB-291; DS-1001

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma . Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively .
    Safusidenib
  • HY-19540
    GSK864
    5+ Cited Publications

    		 Isocitrate Dehydrogenase (IDH) Cancer
    GSK864, a chemical probe, is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
    GSK864
  • HY-18767A
    (R,S)-Ivosidenib

    (R,S)-AG-120

    		 Isocitrate Dehydrogenase (IDH) Inflammation/Immunology Cancer
    (R,S)-Ivosidenib ((R,S)-AG-120) is a (R,S)-enantiomer of Ivosidenib (AG-120) with lower activity. Ivosidenib can be used in research on IDH1-mutant cancers .
    (R,S)-Ivosidenib
  • HY-128888
    (R,R)-GSK321

    		Isocitrate Dehydrogenase (IDH) Cancer
    (R,R)-GSK321 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. (R,R)-GSK321 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity .
    (R,R)-GSK321
  • HY-131312
    Crelosidenib

    LY3410738; Mutant IDH1-IN-6

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
    Crelosidenib
  • HY-N0328R
    alpha-Mangostin (Standard)
    5+ Cited Publications

    α-Mangostin (Standard)

    		 Fungal Reactive Oxygen Species (ROS) Bacterial Apoptosis Virus Protease Reference Standards Cancer
    alpha-Mangostin (Standard) is the analytical standard of alpha-Mangostin. This product is intended for research and analytical applications. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
    alpha-Mangostin (Standard)
  • HY-W017463
    trans-3-(3-Pyridyl)acrylic acid

    		Drug Intermediate TMV Isocitrate Dehydrogenase (IDH) Infection
    trans-3-(3-Pyridyl) acrylic acid is an unsaturated carboxylic acid and synthetic building block, which serves as a synthetic precursor of 3-(3-pyridyl) propanoic acid. trans-3-(3-Pyridyl) acrylic acid can be used to prepare dual mutant IDH1/NAMPT inhibitors and PGE2 antagonist analogs. In addition, trans-3-(3-Pyridyl) acrylic acid exhibits antiviral activity against tobacco mosaic virus (TMV) .
    trans-3-(3-Pyridyl)acrylic acid
  • HY-18717
    Mutant IDH1-IN-2
    2 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    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 IDH1-IN-2
  • HY-128888B
    (S,R)-GSK321

    		Isocitrate Dehydrogenase (IDH) Cancer
    (S,R)-GSK321 is the (S,R)-enantiomer of GSK321 (HY-18948). GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
    (S,R)-GSK321
  • HY-112601
    IDH1 Inhibitor 1

    		Isocitrate Dehydrogenase (IDH) Cancer
    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 IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively . Anticancer activity .
    IDH1 Inhibitor 1
  • HY-112289
    IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    IDH889
  • HY-110144
    TC-E 5008

    		Isocitrate Dehydrogenase (IDH) Cancer
    TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
    TC-E 5008
  • HY-114459
    Mutant IDH1-IN-4

    		Isocitrate Dehydrogenase (IDH) Cancer
    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 .
    Mutant IDH1-IN-4
  • HY-175213
    Mutant IDH1-IN-7

    		Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
    Mutant IDH1-IN-7
  • HY-131312A
    Crelosidenib gentisate

    LY3410738 gentisate; Mutant IDH1-IN-6 gentisate

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes .
    Crelosidenib gentisate
  • HY-100476
    Mutant IDH1-IN-3

    		Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-3 (Compound 1) is a selective allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). Mutant IDH1-IN-3 has an IC50 of 13 nM for R132H IDH1. Mutant IDH1-IN-3 inhibits the production of D-2-hydroxyglutaric acid (2HG) in cells. Mutant IDH1-IN-3 can be used in the study of cancer .
    Mutant IDH1-IN-3
  • HY-158319
    Mutant IDH1/NAMPT-IN-1

    		Apoptosis Isocitrate Dehydrogenase (IDH) NAMPT Cancer
    Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively .
    Mutant IDH1/NAMPT-IN-1
  • HY-149359
    IHMT-IDH1-053

    		Isocitrate Dehydrogenase (IDH) Cancer
    IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
    IHMT-IDH1-053
  • HY-124698
    MRK-A

    		Isocitrate Dehydrogenase (IDH) Cancer
    MRK-A is a selective, blood-brain-barrier permeable mutant IDH1 inhibitor with an IC50 value of 5 nM. MRK-A inhibits 2-HG production. MRK-A has anti-cancer activity against brain tumors .
    MRK-A
  • HY-107977
    IDH1 Inhibitor 3

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1 R132H .
    IDH1 Inhibitor 3
  • HY-143306
    IDH1 Inhibitor 5

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively .
    IDH1 Inhibitor 5
  • HY-143234
    mIDH1-IN-1

    		Isocitrate Dehydrogenase (IDH) Cancer
    mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
    mIDH1-IN-1
  • HY-121736
    AGI-12026

    AGI-026

    		 Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
    AGI-12026
  • HY-112289B
    (1R)-IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    (1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    (1R)-IDH889
  • HY-121916
    ML309

    		Isocitrate Dehydrogenase (IDH) Cancer
    ML309 is a highly selective and potent inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H), with an IC50 of 96 nM. ML309 is a competitive inhibitor of α-KG, with a Ki value of 156 nM, and its inhibitory activity against the wild-type IDH1 is greater than 35 μM. ML309 effectively reduces the production of the tumor metabolite 2-HG in U87MG cells. ML309 can be used as a chemical probe to study the role of the mutant IDH1 in cancer .
    ML309
  • HY-N12390
    Alternaphenol B2

    		Isocitrate Dehydrogenase (IDH) Cancer
    Alternaphenol B2 is a selective IDH1 inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC50 values of 41.9 μM .
    Alternaphenol B2
  • HY-120181
    AGI-14100

    		Isocitrate Dehydrogenase (IDH) Cancer
    AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .
    AGI-14100
  • HY-123153
    GSK990

    		Isocitrate Dehydrogenase (IDH) Cancer
    GSK990 is an inactive mutant IDH1 inhibitor with no significant inhibitory activity against wild-type or mutant IDH1/IDH2 enzymes. In experiments, GSK990 can serve as an inactive negative control for the IDH1 inhibitor GSK321 (HY-18948). GSK990 is applicable to the research of acute myeloid leukemia .
    GSK990
  • HY-104036R
    IDH-305 (Standard)

    		Reference Standards Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 (Standard) is the analytical standard of IDH-305 (HY-104036). This product is intended for research and analytical applications. IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT)) .
    IDH-305 (Standard)
  • HY-104042R
    Vorasidenib (Standard)

    AG-881 (Standard)

    		 Reference Standards Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (Standard) is the analytical standard of Vorasidenib (HY-104042). This product is intended for research and analytical applications. Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
    Vorasidenib (Standard)
  • HY-100020R
    BAY-1436032 (Standard)

    		Isocitrate Dehydrogenase (IDH) Reference Standards Cancer
    BAY-1436032 (Standard) is the analytical standard of BAY-1436032 (HY-100020). This product is intended for research and analytical applications. BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
    BAY-1436032 (Standard)

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