150627-37-5
Chemical Structure
RK-682
- CAS No.: 150627-37-5
- Formula:C21H36O5
- Molecular Weight:368.51
IUPAC Name: (R)-4-hydroxy-5-(hydroxymethyl)-3-palmitoylfuran-2(5H)-one
InChIKey: KZTSLHQKWLYYAC-GOSISDBHSA-N
SMILES: CCCCCCCCCCCCCCCC(C1=C([C@@H](CO)OC1=O)O)=O
Biological Activity: RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[1][2][3].
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RK-682 | RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24. | |||||||||||||||||||||
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References
- [1]. Usui T, et al., Design and synthesis of a dimeric derivative of RK-682 with increased inhibitory activity against VHR, a dual-specificity ERK phosphatase: implications for the molecular mechanism of the inhibition. Chem Biol. 2001 Dec;8(12):1209-20. [Content Brief]
- [2]. Hamaguchi T, et al., RK-682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1phase. FEBS Lett. 1995 Sep 18;372(1):54-8. [Content Brief]
- [3]. Tatsumi Y, et al., Inhibition of Heparanase Expression Results in Suppression of Invasion, Migration and Adhesion Abilities of Bladder Cancer Cells. Int J Mol Sci. 2020 May 27;21(11):3789. [Content Brief]
