SML1757
GSK864
≥98% (HPLC)
别名:
(S)-1-(4-Fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide
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关于此项目
经验公式（希尔记法）:
C30H31FN6O4
化学文摘社编号:
分子量:
558.60
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
InChI key
DUCNNEYLFOQFSW-PMERELPUSA-N
SMILES string
O=C(C1=CC=CN1)N2C[C@@](C(N)=O)(C)C(N(CC3=CC=C(F)C=C3)N=C4C(NC5=CC(C)=C(OC)C(C)=C5)=O)=C4C2
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -66 to -76°, c = 0.5 in methanol
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
GSK864 helps to decrease cell viability and stimulates apoptosis of tumor cells.
GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. It appears that GSK864 binds to an allosteric binding site and locks WT and mutant IDH1s in a catalytically inactive conformation. GSK864 is a highly bioavailable analog of GSK321. For full characterization details, please visit the GSK864 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1).
Features and Benefits
GSK864 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.
This compound is a featured product for Nitric Oxide & Cell Stress research. Click here to discover more featured Nitric Oxide & Cell Stress products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Other Notes
GSK864 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK864 probe summary on the Chemical Probes Portal website.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Cancer-associated IDH1 promotes growth and resistance to targeted therapies in the absence of mutation.
Calvert AE, et al.
Cell Reports, 19(9), 1858-1873 (2017)
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