ptpases

(Rac)-RK-682 is a racemic mixture that functions as a protein tyrosine phosphatases (PTPases) inhibitor, specifically targeting protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B), with inhibitory concentrations (IC50s) of 8.6 μM, 12.4 μM, and 0.7 μM, respectively [1].

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Suramin is a reversible, competitive inhibitor of protein-tyrosine phosphatases (PTPases) [1], demonstrating potent inhibition against sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) [2]. It also acts as a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) [3] [4] and exhibits potent inhibition of SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) [5]. Additionally, Suramin effectively inhibits IP5K, showcasing its antiparasitic, anti-neoplastic, and anti-angiogenic properties [6] [7] [8].

RK-682 is a natural selective inhibitor of protein tyrosine phosphatases (PTPases).