Calcineurin

Tacrolimus (FK506, Axon 2263) is an immunosuppressive agent that suppresses both the immune response and apoptosis through inhibition of the phosphatase activity of calcineurin (calcium dependent serine/threonine protein phosphatase 2B; EC 3.1.3.16). FKBP12, the best-characterized member of the FKBP family of immunophilins, interacts with calcineurin only in the presence of Tacrolimus[1]. Structural studies have shown that the FKBP12–FK506 complex binds 'snugly' to calcineurin and blocks its interaction with substrates. Calcineurin, that is activated by Ca2+ and calmodulin, is implicated in both signal transduction events and apoptosis[2].


[1] C.B. Kang et al. FKBP family proteins: immunophilins with versatile biological functions. Neurosignals. 2008, 16, 318-325.
[2] M. Shirane et al. Inherent calcineurin inhibitor FKBP38 targets Bcl-2 to mitochondria and inhibits apoptosis. Nat. Cell Biol. 2003, 5, 28-37. 


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Axon ID Name Description From price
2480 LW6 Inhibitor of HIF-1α stability via MDH2 inhibition and/or binding with CHP1 €85.00
2263 Tacrolimus Potent Calcineurin (Ca2+ dependent protein phosphatase 2B) inhibitor €100.00

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