GSK864
Synonym(s):(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
- CAS NO.：1816331-66-4
- Empirical Formula: C30H31FN6O4
- Molecular Weight: 558.6
- MDL number: MFCD30478507
- Update Date: 2026-04-24 14:59:00
What is GSK864?
Biochem/physiol Actions
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
Properties of GSK864
| Boiling point: | 782.9±60.0 °C(Predicted) |
| Density | 1.37±0.1 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | DMF:20.0(Max Conc. mg/mL);35.8(Max Conc. mM) DMSO:60.0(Max Conc. mg/mL);107.41(Max Conc. mM) Ethanol:20.0(Max Conc. mg/mL);35.8(Max Conc. mM) Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.9(Max Conc. mM) |
| pka | 11.73±0.70(Predicted) |
| form | powder |
| color | white to beige |
| optical activity | [α]/D -66 to -76°, c = 0.5 in methanol |
Safety information for GSK864
Computed Descriptors for GSK864
New Products
5-bromo-4-fluoro-2-nitrobenzaldehyde (R)-(-)-2-Amino-1-propanol Cyclobutanone Fmoc-OSu 1-(2-Chloroethyl)pyrrolidine Hydrochloride 2-Amino-2-(4-methylphenyl)acetic acid β-Bromostyrene Ethyl 3-phenylpropanoate Phenethyl cinnamate Dipropyl disulfide 4 pentyn 1 ol N-Vinylformamide Methacrylate-PEG-Methacrylate, Mn:35000 2,4-Dihydroxyacetophenone 2-Chloro 5-Fluoro Pyridine Vasicinone 2-Chloroisonicotinic Acid Tween 80 or Polysorbate 80 2-Butyn-1-oL 2-Pentyn-1-oL 4-Nitrobenzotrifluoride N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine Pirtobrutinib intd. N-(4-Cyano-3-(trifluoromethyl)phenyl)-2-methyloxirane-2-carboxamideRelated products of tetrahydrofuran
![N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide](https://img.chemicalbook.in/CAS2/GIF/864082-47-3.gif)
![Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-](https://img.chemicalbook.in/CAS/20211123/GIF/2170137-61-6.gif)
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