Description
- SKU:
- 10-4300-200µg
- CAS Number:
- 150627-37-5
- Extra Details:
- RK-682 is a protein tyrosine phosphatase inhibitor (IC50’s = 54 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 – RK-682 readily forms metal complexes that affects its phosphatase inhibitory activity.6 RK-682 has been identified as a potential promiscuous inhibitor.7
- Molecular Weight:
- 368.52
- Physical State:
- Off-white or Yellow solid
- References:
- 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 al. (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
- Shipping Conditions:
- Ambient
- Storage Conditions:
- -20°C
- Supplier:
- Focus Biomolecules
- Purity:
- 98% by TLC, NMR (Conforms)
- Chemical Name:
- 3-Hexadecanoyl-5-hydroxymethyltetronic acid
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