- A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase.
A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase.
Biochemical and biophysical research communications (2013-03-15)
Satomi Niino, Yutaka Nakamura, Yoshio Hirabayashi, Michiyo Nagano-Ito, Shinichi Ichikawa
PMID23485465
ABSTRACT
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.