RK‐682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1phase
- 18 September 1995
- journal article
- Published by Wiley in FEBS Letters
- Vol. 372 (1) , 54-58
- https://doi.org/10.1016/0014-5793(95)00953-7
Abstract
A specific inhibitor of protein tyrosine phosphatase (PTPase), RK‐682 (3‐hexadecanoyl‐5‐hydroxymethyl‐tetronic acid) was isolated from microbial metabolites. In vitro, RK‐682 inhibited dephosphorylation activity of CD45 and VHR with IC50 54 and 2.0 μM, respectively. In situ, sodium orthovanadate and RK‐682 enhanced the phosphotyrosine level of Ball‐1 cells, a human B cell leukemia, but not the phosphoserine/threonine level. The PTPase inhibitors, however, had the different arrest point on the cell cycle progression. Sodium orthovanadate inhibited the cell cycle progression at G2/M boundary phase, on the other hand, RK‐682 inhibited the G1/S transition.Keywords
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