| Bioactivity | Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD)[1][2][3]. | ||||||||||||
| Invitro | Shield-1 (0.1 nM-1 μM) responses characterization of destabilizing domains[1].Shield-1 (1 μM; 24 h) treatment shows excellent expression on both TRPV5 and YFP when fused the mtFKBP destabilizing domain to either TRPV5 or YFP, and leads to mtFKBP-TRPV5 forming a functional ion channel[2]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | Shield-1 | ||||||||||||
| CAS | 914805-33-7 | ||||||||||||
| Formula | C42H56N2O10 | ||||||||||||
| Molar Mass | 748.90 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Laura A Banaszynski, et al. A rapid, reversible, and tunable method to regulate protein function in living cells using synthetic small molecules. Cell. 2006 Sep 8;126(5):995-1004. [2]. Schoeber JP, et al. Conditional fast expression and function of multimeric TRPV5 channels using Shield-1. Am J Physiol Renal Physiol. 2009 Jan;296(1):F204-11. [3]. Li S, et al. Effects of Shield1 on the viral replication of varicella zoster virus containing FKBP tagged ORF4and 48. Mol Med Rep. 2018 Jan;17(1):763-770. |