(±) RK-682 | Tyrosine phosphatase inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 200 µg | $75.00 | ||
| 1 mg | $295.00 |
(±)-RK-682 (154639-24-4) is a protein tyrosine phosphatase inhibitor (IC50‘s = 54 7 µM for CD45, 2.0 μM for VHR; did not inhibit cdc25B) originally isolated from the fermentation of Streptomyces sp. 88-682.1 Inhibits cell cycle at G1/S. RK-682 has also been shown to inhibit PLA2 (IC50 = 16 μM)2, HIV-1 protease (IC50 = 84 μM)3, and heparanase (IC50 = 17 μM)4. Natural RK-682 (R-isomer) and synthetic racemic material have identical phosphatase activity.5 Care should be taken when using RK-682 in the presence of metal salts – because it readily forms metal complexes that affects its phosphatase inhibitory activity.6 RK-682 has been identified as a potential promiscuous inhibitor.7
References/Citations:
1) Hamaguchi et al. (1995), RK-682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1 phase; FEBS Lett., 372 54
2) Shinagawa et al. (1993), Tetronic acid derivatives, its manufacturing methods and uses; Jpn.Kokai Tokkyo Koho JP 05-43568, 35 1791
3) Roggo et al. (1994), 3-Alkanoyl-5-hydroxymethyl tetronic acid homologues and resistomycin; new inhibitors of HIV-1 protease; J. Antibiot (Tokyo), 47 136
4) Ishida et al. (2004), Structure-based design of a selective heparanase inhibitor as an antimetastatic agent; Mol. Cancer Ther., 3 1069
5) Sodeoka et al1. (1996), Asymmetric synthesis of RK-682 and its analogs, and evaluation of their protein phosphatase inhibitory activities; Tet. Lett., 37 8775
6) Sodeoka et al. (2001), Asymmetric Synthesis of a 3-Acyltetronic Acid Derivative, RK-682, and Formation of Its Calcium Salt during Silica Gel Chromatography; Chem. Pharm. Bull., 49 206
7) Carneiro et al. (2015), Is RK-682 a promiscuous enzyme inhibitor? Synthesis and in vitro evaluation of protein tyrosine phosphatase inhibition of racemic RK-682 and analogues; Eur. J. Med. Chem., 97 42
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
(±)-RK-682 (154639-24-4) is a protein tyrosine phosphatase inhibitor (IC50‘s = 54 7 µM for CD45, 2.0 μM for VHR; did not inhibit cdc25B) originally isolated from the fermentation of Streptomyces sp. 88-682.1 Inhibits cell cycle at G1/S. RK-682 has also been shown to inhibit PLA2 (IC50 = 16 μM)2, HIV-1 protease (IC50 = 84 μM)3, and heparanase (IC50 = 17 μM)4. Natural RK-682 (R-isomer) and synthetic racemic material have identical phosphatase activity.5 Care should be taken when using RK-682 in the presence of metal salts – because it readily forms metal complexes that affects its phosphatase inhibitory activity.6 RK-682 has been identified as a potential promiscuous inhibitor.7
References/Citations:
1) Hamaguchi et al. (1995), RK-682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1 phase; FEBS Lett., 372 54
2) Shinagawa et al. (1993), Tetronic acid derivatives, its manufacturing methods and uses; Jpn.Kokai Tokkyo Koho JP 05-43568, 35 1791
3) Roggo et al. (1994), 3-Alkanoyl-5-hydroxymethyl tetronic acid homologues and resistomycin; new inhibitors of HIV-1 protease; J. Antibiot (Tokyo), 47 136
4) Ishida et al. (2004), Structure-based design of a selective heparanase inhibitor as an antimetastatic agent; Mol. Cancer Ther., 3 1069
5) Sodeoka et al1. (1996), Asymmetric synthesis of RK-682 and its analogs, and evaluation of their protein phosphatase inhibitory activities; Tet. Lett., 37 8775
6) Sodeoka et al. (2001), Asymmetric Synthesis of a 3-Acyltetronic Acid Derivative, RK-682, and Formation of Its Calcium Salt during Silica Gel Chromatography; Chem. Pharm. Bull., 49 206
7) Carneiro et al. (2015), Is RK-682 a promiscuous enzyme inhibitor? Synthesis and in vitro evaluation of protein tyrosine phosphatase inhibition of racemic RK-682 and analogues; Eur. J. Med. Chem., 97 42
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