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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- No. CAS: 150627-37-5
- Fòrmula: C21H36O5
- Peso molecular:368.51
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
>30 μM
Compound: RK-682
|
Cytotoxicity against human adriamycin- resistant MCF7 cells by WST-1 assay
Cytotoxicity against human adriamycin- resistant MCF7 cells by WST-1 assay
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[PMID: 19836230] |
| MCF7 | IC50 |
>30 μM
Compound: RK-682
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Cytotoxicity against human MCF7 cells by WST-1 assay
Cytotoxicity against human MCF7 cells by WST-1 assay
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[PMID: 19836230] |
| MCF7 | IC50 |
>30 μM
Compound: RK-682
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Cytotoxicity against human tamoxifen-resistant MCF7 cells by WST-1 assay
Cytotoxicity against human tamoxifen-resistant MCF7 cells by WST-1 assay
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[PMID: 19836230] |
| MDA-MB-231 | IC50 |
>30 μM
Compound: RK-682
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Cytotoxicity against human MDA-MB-231 cells by WST-1 assay
Cytotoxicity against human MDA-MB-231 cells by WST-1 assay
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[PMID: 19836230] |
Chemical Information
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No. CAS 150627-37-5
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Appearance Solid
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Peso molecular 368.51
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Fòrmula C21H36O5
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Color White to off-white
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SMILES
CCCCCCCCCCCCCCCC(C1=C([C@@H](CO)OC1=O)O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
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Ficha de datos (264 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RK-682 Related Classifications
HY-135564A Related Classifications
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