RK-682 is the calcium salt of 3-hexadecanoyl-5-hydroxymethyl-tetronic acid, a naturally-occurring specific inhibitor of protein tyrosine phosphatase (PTPase). specifically PTP1B. RK-682 is reported to inhibit dephosphorylation activity of CD45 (IC50 = 54 microM) and VHR (IC50 = 2.0 microM), and to arrest cell cycle progress at the G1/S transition. Studies with RK-682 and derivatives have demonstrated efficacy in inhibiting HIV-1 protease activity. RK-682 also displays activity against heparanase function, a protein indicated as operative in tumor cell invasion and angiogenesis.
1. Roggo, B.E., et al. 1994. J. Antibiot. 47: 136-142. PMID: 8150707
2. Hamaguchi, T., et al. 1995. FEBS Lett. 372: 54-58. PMID: 7556642
3. Ishida, K., et al. 2004. Mol. Cancer Ther. 3: 1069-1077. PMID: 15367701
See how others have used RK-682. Click on the entry to view the PubMed entry .
PMID: # 16545563 Na, M. et al. 2006. Bioorg. Med. Chem. Lett. 16: 3061-3064.
PMID: # 15367701 Ishida, K. et al. 2004. Mol. Cancer Ther. 3: 1069-1077.
PMID: # 7783960 Fujii, S. et al. 1995. Neurosci. Lett. 187: 133-136.
PMID: # 7556642 Hamaguchi, T. et al. 1995. FEBS Lett. 372: 54-58.
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