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    InvivoChem Cat #: V4469
    CAS #: 1305115-80-3Purity ≥98%

    Description: PF-04957325 is a novel, highly potent and selective PDE8 inhibitor with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively. PF-04957325 suppresses T cell adhesion to endothelial cells. Despite its robust effect on T cell adhesion, PF-04957325 was over two orders of magnitude less efficient than PICL in suppressing polyclonal Teff cell proliferation, and showed no effect on cytokine gene expression in these cells. More importantly, PDE8 inhibition did not suppress proliferation and cytokine production of myelin-antigen reactive proinflammatory Teff cells in vivo and in vitro. Thus, targeting PDE8 through PF-04957325 selectively regulates Teff cell interactions with endothelial cells without marked immunosuppression of proliferation, while PDE4 inhibition has partially opposing effects. Collectively, our data identify PF-04957325 as a novel function-specific tool for the suppression of Teff cell adhesion and indicate that PDE4 and PDE8 play unique and non-redundant roles in the control of Teff cell functions.

    References:  2016 Aug 23;7:259. 

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    Molecular Weight: 400.38
    Formula: C₁₄H₁₅F₃N₈OS
    CAS No.: 1305115-80-3
    SMILES: NC1=C(N=NN2C[[email protected]]3CN(CC4=NC=CS4)CCO3)C2=NC(C(F)(F)F)=N1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationPF-04957325; PF 04957325; PF04957325

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    Inhibiting PDE8 suppresses Teff cell adhesion to endothelial cells and is reversed by PDE4 inhibition.  2016 Aug 23;7:259.


    Selective inhibition of Teff cell proliferation by PDE4 inhibition in vitro. Proliferation of purified CD4+CD25−Teff cells exposed to PDE inhibitors.  2016 Aug 23;7:259.


    PF-04957325 does not suppress T cell proliferation in response to MOG35−55ex vivo and in vitro. 


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