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.
| 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 | |