SLF

• CAT Number: R019868
• CAS Number: 195513-96-3
• Molecular Formula: C30H40N2O6
• Molecular Weight: 524.7
• Purity: ≥95%
• Storage: -20°C
• InChI: InChI=1S/C30H40N2O6/c1-6-30(2,3)27(33)28(34)32-17-8-7-12-23(32)29(35)38-24(21-10-9-11-22(31)19-21)15-13-20-14-16-25(36-4)26(18-20)37-5/h9-11,14,16,18-19,23-24H,6-8,12-13,15,17,31H2,1-5H3/t23-,24+/m0/s1
• InChIKey: IIDSDBBDZNDWCN-BJKOFHAPSA-N
• SMILES: COc1cc(CCC(OC(=O)[C@@H]2CCCCN2C(=O)C(=O)C(C)(C)CC)c2cccc(N)c2)ccc1OC

FK-<wbr></wbr>506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-<wbr></wbr>506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-<wbr></wbr>dependent protein phosphatase, calcineurin, leading to disruption of T-<wbr></wbr>cell activation. Synthetic ligand of FKBP (SLF) is a cell-<wbr></wbr>permeable analog of FK-<wbr></wbr>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-<wbr></wbr>specific fusion proteins to induce signaling events within a cellular environment. For example, SLF monomers connected with a 10-<wbr></wbr>atom linker activates Fas signaling via Fas-<wbr></wbr>FKBP fusion proteins with an EC50 of 6 nM.

Reference

1.Dumont, F.J. FK506, An immunosuppressant targeting calcineurin function. Current Medicinal Chemistry 7(7), 731-748 (2000).