Formulation: A solid
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
Purity: ≥98%
Formula Markup: C42H56N2O10
Formula Weight: 748,9
Shelf life (days): 1460
CAS Number: 914805-33-7
Notes: 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).{67495} 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.{67496} 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.
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