Biochemical and Biophysical Research Communications 2013-04-05

A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase.

Satomi Niino, Yutaka Nakamura, Yoshio Hirabayashi, Michiyo Nagano-Ito, Shinichi Ichikawa

文献索引：Biochem. Biophys. Res. Commun. 433(2) , 170-4, (2013)

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摘要

HA14-1 is a Bcl-2 inhibitor that is widely used for studies of apoptosis. In the course of searching for a ceramide glucosyltransferase inhibitor that catalyzes the first glycosylation step of glycosphingolipid synthesis, we unexpectedly found that HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively.Copyright © 2013 Elsevier Inc. All rights reserved.