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Merck

SML1757

Sigma-Aldrich

GSK864

≥98% (HPLC)

Sinónimos:

(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

Fórmula empírica (notación de Hill):
C30H31FN6O4
Número de CAS:
Peso molecular:
558.60
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

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

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

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

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Visite la Librería de documentos

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)

Artículos

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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