Shield-1

Shield-1 is a protein stabilizing ligand that prevents the proteosomal degradation of proteins fused to FK-506 binding protein 1A (FKBP12) containing a leucine-to-proline substitution at position 106 (FKBP12L106P). It displays specific binding for the destabilizing domain FKBP12L106P and does not interfere with other measured cell processes. Shield-1 inhibits decreases in fluorescence in NIH3T3 cells stably expressing YFP-FKBP12L106P in a concentration-dependent manner. It increases secretion of IL-2-FKBP12L106P in HCT116 cells stably expressing IL-2-FKBP12L106P when used at a concentration of 1 µM. In vivo, shield-1 (5 and 10 mg/kg every two days) reduces tumor volume in a mouse xenograft model using HCT116 cells stably expressing IL-2-FKBP12L106P.Formal Name: 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-(2S)-2-piperidinecarboxylic acid, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-(4-morpholinyl)ethoxy]phenyl]propyl ester. CAS Number: 914805-33-7. Synonyms: Shld1. Molecular Formula: C42H56N2O10. Formula Weight: 748.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: O=C(N1[C@@H](CCCC1)C(O[C@@H](C2=CC(OCCN3CCOCC3)=CC=C2)CCC4=CC(OC)=C(C=C4)OC)=O)[C@H](C5=CC(OC)=C(C(OC)=C5)OC)CC. InChi Code: InChI=1S/C42H56N2O10/c1-7-33(31-27-38(49-4)40(51-6)39(28-31)50-5)41(45)44-18-9-8-13-34(44)42(46)54-35(16-14-29-15-17-36(47-2)37(25-29)48-3)30-11-10-12-32(26-30)53-24-21-43-19-22-52-23-20-43/h10-12,15,17,25-28,33-35H,7-9,13-14,16,18-24H2,1-6H3/t33-,34-,35+/m0/s1. InChi Key: NMFHJNAPXOMSRX-PUPDPRJKSA-N.