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RK-682

VHR inhibitor
 
BML-PR112-0200 200 µg 115.00 USD
 
BML-PR112-1000 1 mg 480.00 USD
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Replaces Prod. #: ALX-380-205

RK-682 is a novel tyrosine phosphatase inhibitor isolated from Streptomyces sp. It inhibits the dual specificity VHR phosphatase (IC50=2.0µM) selectively over CD45 (IC50=54µM), Cdc25B and PTP1B (IC50~42µM). RK-682 inhibits cell cycle progression of Ball-1 cells at the G1/S transition and enhances ATP-induced long-term potentiation in guinea pig hippocampal CA1 neurons. Shows potent activity against HIV-1 protease.

Product Specification

Formula:C21H36O5
 
MW:368.5
 
CAS:154639-24-4
 
Purity:≥98% (HPLC)
 
Appearance:Pale yellow solid.
 
Solubility:Soluble in DMSO (25mg/ml), 100% ethanol (10mg/ml), methanol or dimethyl formamide.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
 
BML-PR112 structure
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BML-PR112 structure

Product Literature References

The potent inhibitors of protein tyrosine phosphatase 1B from the fruits of Melaleuca leucadendron: A. Saifudin, et al.; Pharmacognosy Res. 8, 38 (2016), Application(s): Positive control, Full Text
Insulin dependent apolipoprotein B degradation and phosphatidylinositide 3-kinase activation with microsomal translocation are restored in McArdle RH7777 cells following serum deprivation: J.D. Sparks, et al.; Biochem. Biophys. Res. Commun. 469, 326 (2015), Application(s): Cell culture , Abstract;
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: T. Usui, et al.; Chem. Biol. 8, 1209 (2001), Abstract;
RK-682, a potent inhibitor of tyrosine phosphatase, arrested the mammalian cell cycle progression at G1phase: T. Hamaguchi, et al.; FEBS Lett. 372, 54 (1995), Abstract;
The mechanism of ATP-induced long-term potentiation involves extracellular phosphorylation of membrane proteins in guinea-pig hippocampal CA1 neurons: S. Fujii, et al.; Neurosci. Lett. 187, 130 (1995), Abstract;
3-Alkanoyl-5-hydroxymethyl tetronic acid homologues and resistomycin: new inhibitors of HIV-1 protease. I. Fermentation, isolation and biological activity: B.E. Roggo, et al.; J. Antibiot. (Tokyo) 47, 136 (1994), Abstract;

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