FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation. SLF is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin. By itself, SLF does not exhibit a significant cellular response. However, homodimers of SLF or heterodimers with another protein ligand, provide a method to promote the dimerization of ligand-specific fusion proteins to induce signaling events within a cellular environment. For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.
- UPC:
- 12350000
- Condition:
- New
- Availability:
- 3 Days
- Weight:
- 1.00 Ounces
- HazMatClass:
- Yes
- WeightUOM:
- LB
- MPN:
- 10007974-5
- CAS:
- 195513-96-3
