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品質等級
化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D -66 to -76°, c = 0.5 in methanol
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
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
生化/生理作用
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
特點和優勢
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.
其他說明
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Cancer-associated IDH1 promotes growth and resistance to targeted therapies in the absence of mutation.
Cell Reports, 19(9), 1858-1873 (2017)
商品
DISCOVER Bioactive Small Molecules for Nitric Oxide & Cell Stress Research
DISCOVER Bioactive Small Molecules for Nitric Oxide & Cell Stress Research
DISCOVER Bioactive Small Molecules for Nitric Oxide & Cell Stress Research
DISCOVER Bioactive Small Molecules for Nitric Oxide & Cell Stress Research
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