10007974 SLF
Synthetic Ligand of FKBP
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Chemical structure definitions are available for many Cayman products. See Chemical Structure Database for details.
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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.1 Synthetic ligand of FKBP (SLF) is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin.2 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.3,2 For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.3
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1
Dumont, F.J. FK506, An immunosuppressant targeting calcineurin function. Current Medicinal Chemistry 7 731-748 (2000).
2
Braun, P.D., Barglow, K.T., Lin, Y., et al. A bifunctional molecule that displays context-dependent cellular activity. J Am Chem Soc 125 7575-7580 (2003).
3
Amara, J.F., Clackson, T., Rivera, V.M., et al. A versatile synthetic dimerizer for the regulation of protein-protein interactions. Proc Natl Acad Sci USA 94 10618-10623 (1997).
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Purchase 10007974 SLF
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Warning This product is not for human or veterinary use.
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Pricing updated 2010-03-20.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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