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Results for "

IDH1+inhibitor

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

1

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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)) [1] .
    IDH-305
  • 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 [1].
    GSK321
  • 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-128661
    IDH1 Inhibitor 2
    4 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Metabolic Disease
    IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor that exerts its activity through covalent modification of His315 with an IC50 value of 110 nM. IDH1 Inhibitor 2 can dose-dependently reduce the intracellular reduced glutamine metabolic flux, thereby affecting cellular metabolic homeostasis. IDH1 Inhibitor 2 can be used to study the role of IDH1 in cellular metabolic regulation and cancer development [1] .
    IDH1 Inhibitor 2
  • 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 [1]. 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

    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 [1].
    Mutant IDH1-IN-1
  • 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 [1].
    (R,R)-GSK321
  • HY-41648
    IDH1 Inhibitor 8

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 8 (91) is isocitrate dehydrogenase 1 (IDH1) inhibitor. IDH1 Inhibitor 8 can be used for the research of cancer [1].
    IDH1 Inhibitor 8
  • 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-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 [1]. Anticancer activity [1].
    IDH1 Inhibitor 1
  • 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 [1].
    (S,R)-GSK321
  • 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 [1] .
    TC-E 5008
  • HY-150238S
    IDH1 Inhibitor 7-d2

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 7-d2 is the deuterium labeled IDH1 Inhibitor 7 (HY-150238). IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC50 of less than 100 nM [1] .
    IDH1 Inhibitor 7-d2
  • HY-150238
    IDH1 Inhibitor 7

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 7 (Compound 88) is an IDH1 inhibitor with an IC50 of less than 100 nM [1].
    IDH1 Inhibitor 7
  • 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 [1].
    MRK-A
  • HY-162631
    IDH1 Inhibitor 9

    		Apoptosis Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity [1].
    IDH1 Inhibitor 9
  • 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 [1].
    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 [1].
    IDH1 Inhibitor 5
  • 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 [1].
    Alternaphenol B2
  • HY-175770
    mIDH1-IN-2

    		Isocitrate Dehydrogenase (IDH) PDK-1 Apoptosis Cancer
    mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma [1].
    mIDH1-IN-2
  • 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 [1].
    GSK990
  • 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)
  • 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)) [1] .
    IDH-305 (Standard)

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