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Literature summary extracted from

  • Yamanaka, K.; Takahashi, Y.; Azuma, Y.; Hantani, Y.
    Assay development and screening for the identification of ganglioside GM3 synthase inhibitors (2020), Biochemistry, 59, 1242-1251 .
    View publication on PubMed

Application

EC Number Application Comment Organism
2.4.3.9 analysis high-throughput scintillation proximity assay to detect GM3S activity to screen GM3S inhibitors. Methods for detecting the activity of GM3S and sialyltransferase ST3Gal3 are established, through direct measurement of the enzyme products using an automatic rapid solid-phase extraction system directly coupled to a mass spectrometer Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.3.9 CMP product inhibition Homo sapiens
2.4.3.9 N-[5-methyl-1-[2-(morpholin-4-yl)ethyl]-2-oxo-2,3-dihydro-1H-indol-3-yl]acetamide mixed mode of inhibition Homo sapiens
2.4.3.9 [4-[(4-methylbenzene-1-sulfonyl)imino]-1,3,5-triazinan-1-yl]acetic acid mixed mode of inhibition Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.3.9 Homo sapiens Q9UNP4
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.3.9 beta-D-Gal-(1->4)-beta-D-Glc-(1->1)-Cer(d18:1(4E)) + CMP-N-acetyl-beta-neuraminate
-
 Homo sapiens CMP + ganglioside GM3 (d18:1(4E)) + H+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.3.9 GM3S
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.3.9 0.013
-
 pH 6.5, 23°C Homo sapiens [4-[(4-methylbenzene-1-sulfonyl)imino]-1,3,5-triazinan-1-yl]acetic acid
2.4.3.9 0.0156
-
 pH 6.5, 23°C Homo sapiens N-[5-methyl-1-[2-(morpholin-4-yl)ethyl]-2-oxo-2,3-dihydro-1H-indol-3-yl]acetamide
2.4.3.9 0.0887
-
 pH 6.5, 23°C Homo sapiens CMP