A general inhibitor of DUBs
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PR-619

Item No. 16276

Technical Information
Formal Name
thiocyanic acid, C,C'-(2,6-diamino-3,5-pyridinediyl) ester
CAS Number
2645-32-1
Synonyms
  • 2,6-Diamino-3,5-dithiocyanopyridine
  • DUB Inhibitor V
Molecular Formula
C7H5N5S2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 10 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
220, 266, 320 nm
SMILES
NC1=NC(N)=C(SC#N)C=C1SC#N
InChi Code
InChI=1S/C7H5N5S2/c8-2-13-4-1-5(14-3-9)7(11)12-6(4)10/h1H,(H4,10,11,12)
InChi Key
ZXOBLNBVNROVLC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PR-619 is a general inhibitor of deubiquitylating enzymes (DUBs), significantly reducing the activity of a panel of DUBs with EC50 values ranging from 5-20 µM.1 It is cell-permeable and reversible in its action.1 It is selective for DUBs over other proteases.1 PR-619 induces the accumulation of polyubiquitinated proteins in cells, including those not involved in the ubiquitin-proteasome system.2 It is used to study the role of DUBs in diverse pathways, including protein turnover and neurodegeneration.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Altun, M., Kramer, H.B., Willems, L.I., et alActivity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem. Biol. 18(11), 1401-1412 (2011).

    2. Udeshi, N.D., Mani, D.R., Eisenhaure, T., et alMethods for quantification of in vivo changes in protein ubiquitination following proteasome and deubiquitinase inhibition. Mol. Cell. Proteomics 11(15), 148-159 (2012).

    3. Balut, C.M., Loch, C.M., and Devor, D.C. Role of ubiquitylation and USP8-dependent deubiquitylation in the endocytosis and lysosomal targeting of plasma membrane KCa3.1. The FASEB Journal 25(11), 3938-3948 (2011).

    4. Seiberlich, V., Goldbaum, O., Zhukareva, V., et alThe small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: Implications for neurodegenerative diseases. Biochim. Biophys. Acta 1823(11), 2057-2068 (2012).

    5. Bertuccio, C.A., Lee, S.L., Wu, G., et alAnterograde trafficking of KCa3.1 in polarized epithelia is Rab1- and Rab8-dependent and recycling endosome-independent. PLoS One 9(3), 1-16 (2014).