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GSK2807 Trifluoroacetate

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GSK2807 Trifluoroacetate Basic information

Product Name:
GSK2807 Trifluoroacetate
Synonyms:
  • GSK2807 Trifluoroacetate
  • CS-2876
  • (S)-2-Amino-4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-(dimethylamino)propyl)amino)butanoic acid 2,2,2-trifluoroacetic acid salt
  • GSK2807 TFA
  • GSK2807,Inhibitor,GSK2807 Trifluoroacetate,inhibit,GSK-2807 Trifluoroacetate,Histone Methyltransferase,GSK 2807,GSK-2807
CAS:
2245255-66-5
MF:
C21H33F3N8O7
MW:
566.54
EINECS:
604-604-1
Mol File:
2245255-66-5.mol
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GSK2807 Trifluoroacetate Chemical Properties

storage temp. 
under inert gas (nitrogen or Argon) at 2–8 °C
solubility 
DMSO:250.0(Max Conc. mg/mL);441.28(Max Conc. mM)
Water:50.0(Max Conc. mg/mL);88.26(Max Conc. mM)
form 
Solid
color 
White to yellow
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GSK2807 Trifluoroacetate Usage And Synthesis

Uses

GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM[1][2].

IC 50

SMYD3: 14 nM (Ki); SMYD3: 130 nM (IC50)

References

[1] Van Aller GS, et al. Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets. Structure. 2016 May 3;24(5):774-781. DOI:10.1016/j.str.2016.03.010
[2] Kaniskan Hü, et al. Inhibitors of Protein Methyltransferases and Demethylases. Chem Rev. 2018 Feb 14;118(3):989-1068. DOI:10.1021/acs.chemrev.6b00801

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