Shield-1
(Synonyms: Shld1) 目录号 : GC38060
Shield-1是一种特异性、细胞可渗透的FK506结合蛋白-12 (FKBP)配体。
Cas No.:914805-33-7
Sample solution is provided at 25 µL, 10mM.
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Shield-1 is a specific, cell-permeable ligand for FK506-binding protein 12 (FKBP)[1]. Shield-1 reverses the instability of mutated FKBP by binding to FKBP, allowing for the conditional expression of the mtFKBP fusion protein[2]. Shield-1 can influence viral replication by modulating the stability of the mtFKBP fusion protein[3]. Shield-1 is also a commonly used gene-editing tool with the function of erasing RNA N6-methyladenosine modifications[4].
In vitro, treatment of NIH3T3 cells stably expressing the FKBP L106P fusion protein with Shield-1 (1µM) for 24 hours significantly reversed the protein degradation mediated by the destabilizing domain, restored the expression levels of RhoA and Cdc42 proteins, and induced stress fiber formation and pseudopod extension[5]. Treatment of HEK293 cells expressing the mtFKBP-TRPV5 fusion protein with Shield-1 (1µM) for 24 hours significantly reversed the protein degradation mediated by the mtFKBP domain, restoring the cell membrane expression and functional activity of the TRPV5 ion channel[6].
In vivo, systemic administration of Shield-1 (1µM) via the aquatic environment (water dosing) was used to stabilize a systemic DD-YFP fusion protein in Transgenic Medaka fish from the embryonic to adult stages. Shield-1 induced YFP reporter gene expression in a concentration-dependent manner in various organs, including the brain, gills, intestine, liver, kidney, spleen, heart, and gonads. Shield-1 effectively crossed the blood-brain barrier and successfully achieved protein stabilization in germ cells[7].
References:
[1] Madsen D, Jørgensen FP, Palmer D, et al. Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12. ACS Comb Sci. 2020 Mar 9;22(3):156-164.
[2] Li X, Wang S, Li Q, et al. A Rapid and Reversible Molecular "Switch" Regulating Protein Expression in Chlamydomonas reinhardtii. Plant Cell Environ. 2025 Jun;48(6):3913-3924.
[3] Schleiss MR, Fernández-Alarcón C, Bierle CJ, et al. Replication-deficient whole-virus vaccines against cytomegalovirus induce protective immunity in a guinea pig congenital infection model. J Virol. 2025 Jul 22;99(7):e0020725.
[4] Xu Y, Wang Y, Liang FS. Site-Specific m6 A Erasing via Conditionally Stabilized CRISPR-Cas13b Editor. Angew Chem Int Ed Engl. 2023 Oct 23;62(43):e202309291.
[5] Banaszynski LA, Chen LC, Maynard-Smith LA, 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.
[6] Schoeber JP, van de Graaf SF, Lee KP, 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.
[7] Froschauer A, Kube L, Kegler A, et al. Tunable Protein Stabilization In Vivo Mediated by Shield-1 in Transgenic Medaka. PLoS One. 2015 Jul 6;10(7):e0131252.
Shield-1是一种特异性、细胞可渗透的FK506结合蛋白-12 (FKBP)配体[1]。通过与突变的FKBP结合而逆转其不稳定性，允许mtFKBP融合蛋白的条件表达[2]。Shield-1可通过调节mtFKBP融合蛋白的稳定性来影响病毒复制[3]。Shield-1还是一种常用的基因编辑工具，具有擦除RNA N6-甲基腺苷修饰的功能[4]。
在体外，Shield-1（1μM）处理稳定表达FKBP L106P融合蛋白的NIH3T3细胞24小时，可显著逆转由Dstabilizing domain 介导的蛋白降解作用，恢复RhoA、Cdc42蛋白的表达水平，并诱导细胞应力纤维形成、伪足延伸[5]。Shield-1（1μM）处理表达mtFKBP-TRPV5融合蛋白的HEK293细胞24小时，显著逆转由mtFKBP结构域介导的蛋白降解作用，恢复TRPV5离子通道的细胞膜表达及功能活性[6]。
在体内，Shield-1（10nM, 100nM, and 1µM）通过水体给药进行全身性处理，用于稳定Transgenic Medaka fish从胚胎到成鱼各发育阶段的全身性DD-YFP融合蛋白。Shield-1以浓度依赖的方式显著诱导了包括脑、鳃、肠、肝、肾、脾、心脏及性腺在内的多种器官中YFP报告基因的表达，并有效穿过血脑屏障，且在生殖细胞中成功实现蛋白稳定化[7]。
| Cell experiment [1]: | |
Cell lines | HEK293 cells (human embryonic kidney cell line), NIH3T3 cells (mouse embryonic fibroblast cell line), HeLa cells (human epithelial immortal cell line) |
Preparation Method | Cells were transfected to express a fusion protein consisting of a protein of interest (TRPV5 ion channel, YFP, RhoA, Cdc42) tagged with a mutant FK506-binding protein (FKBP) destabilizing domain (DD). Cells were maintained in appropriate culture medium supplemented with serum. The expression of the DD-fused protein is constitutively degraded by the ubiquitin-proteasome system under standard conditions. Shield-1 was applied at concentrations ranging from 0.1nM to 1μM, with 1μM being a commonly used effective concentration. |
Reaction Conditions | 0.1nM to 1μM; 24h |
Applications | Shield-1 treatment rapidly stabilizes the DD-fused protein, preventing its degradation. This leads to the restoration of specific protein functions, such as TRPV5 ion channel activity (evidenced by increased Na⁺ and Ca²⁺ current densities) or induction of specific cellular phenotypes like stress fiber formation. This effect is dose-dependent, reversible upon Shield-1 withdrawal (with a protein half-life of approximately 2-3 hours), and can be repeated over multiple cycles |
| Animal experiment [2]: | |
Animal models | Transgenic Medaka fish (Oryzias latipes) |
Preparation Method | Transgenic fish were generated by microinjection of transposase mRNA and plasmid pDS-actb-DD-YFP into 1-cell stage embryos. Shield-1 (10nM, 100nM, and 1µM) stock solution was dissolved in absolute ethanol and administered directly to the aquarium water. |
Dosage form | 10nM, 100nM, and 1µM; added to water |
Applications | Shield-1 administration led to a rapid, concentration-dependent, and reversible stabilization of the DD-YFP fusion protein in vivo. Induction was observed ubiquitously in various organs (brain, liver, testis, gills, gut, kidney, spleen, heart) throughout the animal's life, including successful crossing of the blood-brain barrier and effective targeting of gonadal stem cells (spermatogonia in testis). The system allowed for fine-tuning of protein expression levels. |
References: | |
| Cas No. | 914805-33-7 | SDF | |
| 别名 | Shld1 | ||
| Canonical SMILES | O=C([C@H]1N(C([C@H](C2=CC(OC)=C(OC)C(OC)=C2)CC)=O)CCCC1)O[C@@H](C3=CC=CC(OCCN4CCOCC4)=C3)CCC5=CC=C(OC)C(OC)=C5 | ||
| 分子式 | C42H56N2O10 | 分子量 | 748.9 |
| 溶解度 | DMSO: ≥ 250 mg/mL (333.82 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3353 mL | 6.6765 mL | 13.3529 mL |
| 5 mM | 267.1 μL | 1.3353 mL | 2.6706 mL |
| 10 mM | 133.5 μL | 667.6 μL | 1.3353 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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