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Literature summary for 2.4.1.80 extracted from

  • Niino, S.; Nakamura, Y.; Hirabayashi, Y.; Nagano-Ito, M.; Ichikawa, S.
    A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase (2013), Biochem. Biophys. Res. Commun., 433, 170-174.
    View publication on PubMed
Search for more literature for 2.4.1.80

Inhibitors

Inhibitors Comment Organism Structure
ethyl-2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate i.e. HA14-1, a reversible small molecule Bcl-2 inhibitor that also inhibits GlcT-1 enzyme activity. HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively. HA-14 does not possess structural homology with the substrates UDP-glucose and ceramide. Possible binding of GlcT-1 to Bcl-2 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16739
-
-

Source Tissue

Source Tissue Comment Organism Textmining
B-16 cell
-
 Homo sapiens
-
melanoma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-glucose + 6-(((N-7-nitrobenz-2-oxa-1,3-diazol-4yl)amino)caproyl)sphingosine
-
 Homo sapiens UDP + ?
-
 ?

Synonyms

Synonyms Comment Organism
GlcT-1
-
 Homo sapiens
UDP-glucose: ceramide glucosyltransferase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0045
-
 ethyl-2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate pH 7.5, 30°C Homo sapiens

General Information

General Information Comment Organism
additional information the use of ethyl-2-amino-6-bromo-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate, i.e. HA14-1, as a Bcl-2 inhibitor in studies of apoptosis might produce misleading results, because HA14-1 can also affect a ceramide-mediated cell death pathway by inhibiting GlcT-1. Bcl-2 is a protein factor known to suppress apoptosis by binding and inactivating pro-apoptotic proteins such as Bax and BH3-only family proteins Homo sapiens