General Description

• Tacrolimus is a macrolide isolated from Streptomyces tsukubaensis, that shows immunosuppressant, neuroprotective, and neuroregenerative activities, having the ability to block T-cell proliferation and activation in response to antigenic or mitogenic stimulation

• Tacrolimus interacts with the immunophilins cyclophilin and FKBP-12. Tacrolimus binds to the FKBP-12 protein (FK506 binding protein) and forms a complex with calcium-dependent proteins. This FKBP12-FK506 complex inhibits calcineurin phosphatase activity, resulting in decreased cytokine production, inhibition of T-lymphocyte signal transduction

• Tacrolimus also inhibits the transcription for genes that encode IL-3, IL-4, IL-5, GM-CSF, and TNF, all of which are involved in the early stages of T-cell activation

• This compound can also inhibit the release of pre-formed mediators from skin mast cells and basophils and downregulate the expression of FceRI on Langerhans cells

Application

• Tacrolimus has been studied in vitro to understand its impact on neutrophil production and/or survival • It is applied to suppress the inflammation in ulcerative cells

• It is used as a research tool in chemically induced dimerization applications in biology

• It has been used in in vitro studies to investigate its effect on human monocyte-derived dentritic cells

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