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Mutant-IDH1- Inhibitor

" in MedChemExpress (MCE) Product Catalog:

16

Inhibitors & Agonists

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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.
    <em>Mutant IDH1</em> <em>inhibitor</em>
  • HY-114459

    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-18082
    AGI-5198
    Maximum Cited Publications
    11 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-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-145594

    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-12475
    Mutant IDH1-IN-1
    2 Publications Verification

    Isocitrate Dehydrogenase (IDH) Cancer
    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.
    Mutant IDH1-IN-1
  • HY-131312

    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 .
    LY3410738
  • HY-18948
    GSK321
    1 Publications Verification

    GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia .
    GSK321
  • HY-N0328
    alpha-Mangostin
    3 Publications Verification

    α-Mangostin

    Reactive Oxygen Species 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-143306

    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 .
    <em>IDH1</em> <em>Inhibitor</em> 5
  • HY-121736

    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-112601

    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 .
    <em>IDH1</em> <em>Inhibitor</em> 1
  • HY-N0328R

    α-Mangostin (Standard)

    Fungal Reactive Oxygen Species Bacterial Apoptosis Virus Protease 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-110144

    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-104036

    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-128888B

    Isocitrate Dehydrogenase (IDH) Cancer
    (S,R)-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. (S,R)-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. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
    (S,R)-GSK321

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