Shield-1
Based on 11 publication(s) in Google Scholar
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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.55%
- No. CAS: 914805-33-7
- Fòrmula: C42H56N2O10
- Peso molecular:748.90
-
Almacenamiento:
-80°C, stored under nitrogen
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Shield-1
More- Nature. 2025 Feb;638(8050):519-527. [Abstract]
- Nat Commun. 2026 Mar 5;17(1):2160. [Abstract]
- Nat Commun. 2025 Nov 20;16(1):10127. [Abstract]
- Nat Commun. 2023 Dec 11;14(1):8187. [Abstract]
- Cell Rep. 2024 Sep 14;43(9):114738. [Abstract]
- STAR Protoc. 2025 Feb 10;6(1):103634. [Abstract]
- bioRxiv. 2026 Jun 19.
- bioRxiv. 2026 Jan 29:2026.01.27.702006. [Abstract]
- bioRxiv. 2025 May 19.
- bioRxiv. 2024 Feb 17.
- bioRxiv. 2024 Feb 16.
Customer Validation & Images
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
Cell Imaging/Staining
-
IF
-
2D/3D Cell Culture and Differentiation
Actividad biológica
|
FKBP12 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | EC50 |
100 nM
Compound: shield-1
|
Binding affinity to human FKBP F36V/L106P mutant-YFP fusion protein expressed in NIH3T3 cells after 24 hrs
Binding affinity to human FKBP F36V/L106P mutant-YFP fusion protein expressed in NIH3T3 cells after 24 hrs
|
[PMID: 18039574] |
| NIH3T3 | EC50 |
60 nM
Compound: shield-1
|
Stability of FKBP12 V2A mutant-YFP fusion protein expressed in NIH3T3 cells after 24 hrs by flow cytometry
Stability of FKBP12 V2A mutant-YFP fusion protein expressed in NIH3T3 cells after 24 hrs by flow cytometry
|
[PMID: 17603093] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NIH3T3 cells
-
Concentration:0.1 nM-1 μM
-
Incubation Time:
-
Result:Stabilized the YFP fusion protein of L106P by higher concentrations of Shld1 (EC50∼100 nM).
-
Cell Line:HEK293 cells[2]
-
Concentration:1 μM
-
Incubation Time:24 hours
-
Result:Expressed both TRPV5 and YFP well when Shield-1 in the medium, whereas in the abscence of Shield-1 decreased TRPV5 or YFP protein expression.
Chemical Information
-
No. CAS 914805-33-7
-
Appearance Solid
-
Peso molecular 748.90
-
Fòrmula C42H56N2O10
-
Color White to yellow
-
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
-
Synonyms
Shld1
-
Envío
Shipping with dry ice.
-
Almacenamiento
-80°C, stored under nitrogen
Publications (11)
-
Journal Impact Factor
-
Most Recent
-
Nature
2025 Feb;638(8050):519-527. PMID: 39880951
Shield-1 purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):519-527. [Abstract]
Identification of proteome changes after acute induction of FBXO31(D334N) expression. FBXO31-knockout cells were stably transduced with ligand-inducible DD-FBXO31(D334N). The total protein abundance was measured by tandem-mass-tag MS after 12 h of protein induction (2 µM Shield-1) and compared to shield-treated parental cells.
Shield-1 purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):519-527. [Abstract]
Comparison of proteome-wide responses to FBXO31 induction for wild-type or D334N mutant DD-3xFLAG-FBXO31 induced by 12 h of treatment with Shield-1 (2 μM; 12 h) measured by TMT-MS.
-
Nat Commun
TCL1A mediates DNA methylation defects in recurrent hydatidiform mole with NLRP7 pathogenic variants. [Abstract]2026 Mar 5;17(1):2160. PMID: 41786744 -
Nat Commun
2025 Nov 20;16(1):10127. PMID: 41266351
Shield-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 20;16(1):10127. [Abstract]
Representative micrographs of fixed RPE-1 cells stably expressing MCPH1-BRCT-eGFP treated with Shield-1 (1 μM) and Doxycycline (Dox) for 12 h and transfected with sgRNAs targeting 1 or 4 genomic locations for 7–8 h. A plasmid without sgRNA was used as a control. Cells were stained with anti-Cas9 (gray) and anti-γH2AX (red), and nuclei were co-stained with DAPI. Nuclear masks, based on DAPI signal, are shown. Scale bars: 5 µm.
-
Nat Commun
GRAF1 integrates PINK1-Parkin signaling and actin dynamics to mediate cardiac mitochondrial homeostasis. [Abstract]2023 Dec 11;14(1):8187. PMID: 38081847 -
Cell Rep
2024 Sep 14;43(9):114738. PMID: 39277864
Shield-1 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Sep 14;43(9):114738. [Abstract]
Immunofluorescent microscopy of hTERT-RPE1 p53−/− Cas9 cells stably expressing DD-HA-ER-I-PpoI + DMSO or Shield-1 (2 μM; 6 h) + 4-OHT for 6 h. Dashed boxes show zoomed inlet. Green, endogenous TCOF1; blue, DAPI; nucleus outlined with dashed lines; nucleoli, gray dashed circles. Scale bars, 10 μm.
Shield-1 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Sep 14;43(9):114738. [Abstract]
Clonogenic survival assay of hTERT-RPE1 p53−/− DD-HA-ER-I-PpoI cells transduced with sgRNAs targeting different genes of the UFMylation pathway. Cells were treated with DMSO or Shield-1 (100 nM) + 4-OHT every 3 days for a total of 10-14 days and then stained with crystal violet.
Shield-1 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Sep 14;43(9):114738. [Abstract]
Western blot analysis of total ATM, phospho-ATM S1981, UFL1, and GAPDH protein levels in LacZ transduced hTERT-RPE1 p53−/− Cas9 DD-HA-ER-I-PpoI or UFL1 KO cells + DMSO or Shield-1 + 4-OHT over 6 h.
-
STAR Protoc
2025 Feb 10;6(1):103634. PMID: 39937649 -
-
bioRxiv
Precision CRISPR annotation of the functional enhancer landscape in primary human T cells. [Abstract]2026 Jan 29:2026.01.27.702006. PMID: 41659577 -
-
-
Solvente y solubilidad
DMSO : 67.5 mg/mL (90.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5.25 mg/mL (7.01 mM); Clear solution
This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5.25 mg/mL (7.01 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (280 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3353 mL | 6.6765 mL | 13.3529 mL | 33.3823 mL |
| 5 mM | 0.2671 mL | 1.3353 mL | 2.6706 mL | 6.6765 mL | |
| 10 mM | 0.1335 mL | 0.6676 mL | 1.3353 mL | 3.3382 mL | |
| 15 mM | 0.0890 mL | 0.4451 mL | 0.8902 mL | 2.2255 mL | |
| 20 mM | 0.0668 mL | 0.3338 mL | 0.6676 mL | 1.6691 mL | |
| 25 mM | 0.0534 mL | 0.2671 mL | 0.5341 mL | 1.3353 mL | |
| 30 mM | 0.0445 mL | 0.2225 mL | 0.4451 mL | 1.1127 mL | |
| 40 mM | 0.0334 mL | 0.1669 mL | 0.3338 mL | 0.8346 mL | |
| 50 mM | 0.0267 mL | 0.1335 mL | 0.2671 mL | 0.6676 mL | |
| 60 mM | 0.0223 mL | 0.1113 mL | 0.2225 mL | 0.5564 mL | |
| 80 mM | 0.0167 mL | 0.0835 mL | 0.1669 mL | 0.4173 mL |
Shield-1 Related Classifications
HY-112210 Related Classifications
Powered by Bioz