RK-682A specific PTP1B inhibitor

RK-682 (CAS 332131-32-5)

RK-682 | CAS 332131-32-5 is rated 5.0 out of 5 by 1.
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Application: A specific PTP1B inhibitor
CAS Number: 332131-32-5
Purity: >95%
Molecular Weight: 775.06
Molecular Formula: (C21H35O5)2•Ca
* Refer to Certificate of Analysis for lot specific data (including water content).
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RK-682 is the calcium salt of 3-hexadecanoyl-5-hydroxymethyl-tetronic acid, a naturally-occurring specific inhibitor of protein tyrosine phosphatase (PTPase). specifically PTP1B. RK-682 is reported to inhibit dephosphorylation activity of CD45 (IC50 = 54 microM) and VHR (IC50 = 2.0 microM), and to arrest cell cycle progress at the G1/S transition. Studies with RK-682 and derivatives have demonstrated efficacy in inhibiting HIV-1 protease activity. RK-682 also displays activity against heparanase function, a protein indicated as operative in tumor cell invasion and angiogenesis.


References

1. Roggo, B.E., et al. 1994. J. Antibiot. 47: 136-142. PMID: 8150707
2. Hamaguchi, T., et al. 1995. FEBS Lett. 372: 54-58. PMID: 7556642
3. Ishida, K., et al. 2004. Mol. Cancer Ther. 3: 1069-1077. PMID: 15367701

Physical State :
Solid
Derived From :
Streptomyces sp.
Solubility :
Soluble in ethanol, methanol, DMF, and DMSO.
Storage :
Store at -20° C
IC50 :
CD45 dephosphorylation activity: IC50 = 54 mM; VHR dephosphorylation activity: IC50 = 2 mM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

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RK-682  Product Citations

See how others have used RK-682. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 16545563  Na, M. et al. 2006. Bioorg. Med. Chem. Lett. 16: 3061-3064.

PMID: # 15367701  Ishida, K. et al. 2004. Mol. Cancer Ther. 3: 1069-1077.

PMID: # 7783960  Fujii, S. et al. 1995. Neurosci. Lett. 187: 133-136.

PMID: # 7556642  Hamaguchi, T. et al. 1995. FEBS Lett. 372: 54-58.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Na Na, M. et al. (PubMed 16545563) used RK-682, an inhibitor of protein tyrosine phosphatase (PTP), as a positive control against other potential PTP inhibitors. -SCBT Publication Review
Date published: 2015-06-08
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