SML0839
AGI-5198
≥98% (HPLC)
别名:
IDH-C35, N-Cycohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide, N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide
InChI
1S/C27H31FN4O2/c1-19-9-6-7-14-24(19)26(27(34)30-22-11-4-3-5-12-22)32(23-13-8-10-21(28)17-23)25(33)18-31-16-15-29-20(31)2/h6-10,13-17,22,26H,3-5,11-12,18H2,1-2H3,(H,30,34)
InChI key
FNYGWXSATBUBER-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 3 mg/mL, clear
storage temp.
2-8°C
Application
AGI-5198 has been used as a negative control in ligand dilution series.
Biochem/physiol Actions
AGI-5198 is a highly potent and selective mutant IDH1 inhibitor.
AGI-5198 is a highly potent and selective mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
In human chondrosarcoma cell line JJ012, AGI-5198 promotes apoptosis and G2/M cell cycle arrest. It also prevents the generation of colony in chondrosarcoma cell lines. AGI-5198 hinders the multiplication of cell and induces demethylation of H3K9me3 and H3K27me3.
Other Notes
AGI-5198 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the AGI-5198 probe summary on the Chemical Probes Portal website.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Luyuan Li et al.
PloS one, 10(9), e0133813-e0133813 (2015-09-15)
Chondrosarcomas are malignant bone tumors that produce cartilaginous matrix. Mutations in isocitrate dehydrogenase enzymes (IDH1/2) were recently described in several cancers including chondrosarcomas. The IDH1 inhibitor AGI-5198 abrogates the ability of mutant IDH1 to produce the oncometabolite D-2 hydroxyglutarate (D-2HG)
Near-native, site-specific and purification-free protein labeling for quantitative protein interaction analysis by MicroScale Thermophoresis.
Bartoschik T, et al.
Scientific Reports, 8(1), 4977-4977 (2018)
Frontiers in Clinical Drug Research, 495-495 (2016)
Geon-Hee Kim et al.
International journal of molecular sciences, 20(11) (2019-06-04)
The R132H mutation in isocitrate dehydrogenase 1 (IDH1R132H) is commonly observed and associated with better survival in glioblastoma multiforme (GBM), a malignant brain tumor. However, the functional role of IDH1R132H as a molecular target for GBM treatment is not completely
Kancharana Bala Bhaskara Rao et al.
FEBS letters, 593(16), 2177-2193 (2019-06-19)
Isocitrate dehydrogenases (IDHs) are metabolic enzymes that are mutated in several cancers, resulting in overproduction of d-2-hydroxyglutarate (D-2HG). However, the signalling pathways and factors that regulate mutant IDHs or their metabolites remain elusive. Here, we report that in synchronized cells
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