RK-682 (hemicalcium)

RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A) . RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium 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 hemicalcium 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].

Product Specifications

CAS Number

[332131-32-5]

UNSPSC

12352005

Target

Autophagy; ERK; HIV Protease; Phosphatase; Phospholipase

Type

Reference compound

Related Pathways

Anti-infection; Autophagy; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Stem Cell/Wnt

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/rk-682-hemicalcium.html

Solubility

10 mM in DMSO

Smiles

CCCCCCCCCCCCCCCC(C1=C([C@@H](CO)OC1=O)O)=O.[1/2].[Ca]

Molecular Formula

C21H36O5.1/2Ca

Molecular Weight

408.59

References & Citations

[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.|[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. |[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.