Art. -Nr.: HY-112210

Shield-1

(Synonyms: Shld1)

11 Cited Publications

Kundenbewertung

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).

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Reinheit: 99.55%
CAS. Nr.: 914805-33-7
Formel: C₄₂H₅₆N₂O₁₀
Molecular Weight:748.90

Speicherung:

-80°C, stored under nitrogen

Shield-1 Chemical Structure

CAS. Nr.: 914805-33-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

FKBP12

Cellular Effect

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]

In Vitro

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.

Western Blot Analysis^[1]

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).

Western Blot Analysis^[2]

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

CAS. Nr. 914805-33-7
Appearance Solid
Molecular Weight 748.90
Formel 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
Versand

Shipping with dry ice.
Speicherung

-80°C, stored under nitrogen

Publications (11)

All Cell Imaging/StainingIFBio/Physico-chemical Assay2D/3D Cell Culture and DifferentiationWB

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Journal Impact Factor

Nature

C-terminal amides mark proteins for degradation via SCF-FBXO31. [Abstract]

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

Engineered chromatin readers track damaged chromatin dynamics in live cells and animals. [Abstract]

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

Protein UFMylation regulates early events during ribosomal DNA-damage response. [Abstract]

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

Protocol for the purification and analysis of nuclear UFMylated proteins. [Abstract]

2025 Feb 10;6(1):103634. PMID: 39937649
bioRxiv

2026 Jun 19.
bioRxiv

Precision CRISPR annotation of the functional enhancer landscape in primary human T cells. [Abstract]

2026 Jan 29:2026.01.27.702006. PMID: 41659577
bioRxiv

2025 May 19.
bioRxiv

2024 Feb 17.
bioRxiv

2024 Feb 16.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3353 mL

6.6765 mL

13.3529 mL

5 mM

0.2671 mL

1.3353 mL

2.6706 mL

10 mM

0.1335 mL

0.6676 mL

1.3353 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5.25 mg/mL (7.01 mM); Clear solution

This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Shield-1

11 Cited Publications

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Shield-1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Shield-1

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Shield-1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Shield-1

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Shield-1 Related Classifications

HY-112210 Related Classifications