RK-682

BML-PR112

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VHR inhibitor

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.

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Product Details

Appearance	Pale yellow solid.
CAS	154639-24-4
Couple Target	Serine/threonine-protein phosphatase
Couple Type	Inhibitor
Formula	C₂₁H₃₆O₅
MW	368.5
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO (25mg/ml), 100% ethanol (10mg/ml), methanol or dimethyl formamide.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

The potent inhibitors of protein tyrosine phosphatase 1B from the fruits of Melaleuca leucadendron: A. Saifudin, et al.; Pharmacognosy Res. 8, S38 (2016), Application(s): Positive control, Abstract — 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
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
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
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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RK-682

BML-PR112

Product Details

Handling & Storage

Datasheet, Manuals, SDS & CofA

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