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Merck

SML1757

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C30H31FN6O4
分子量:
558.60
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

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

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


分析证书(COA)

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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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