Shield-1 (Synonyms: Shld1)

Name: Shield-1
Brand: MedChemExpress
SKU: HY-112210
Rating: 5.0 (10 reviews)

Cat. No.: HY-112210 Purity: 99.73%: Data Sheet
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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).

For research use only. We do not sell to patients.

CAS No. : 914805-33-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 10 publication(s) in Google Scholar

10 Publications Citing Use of MCE Shield-1

Cell Imaging/Staining

Bio/Physico-chemical Assay

2D/3D Cell Culture and Differentiation

: 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.

: 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.

: 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.

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Description

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.

Molecular Weight

748.90

Formula

C₄₂H₅₆N₂O₁₀

CAS No.

914805-33-7

Appearance

Solid

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

Shipping

Shipping with dry ice.

Storage

-80°C, stored under nitrogen

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.73%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (257 KB) HNMR (286 KB) RP-HPLC (254 KB) LCMS (85 KB)

Handling Instructions (2659 KB)

References

[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

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

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Shield-1914805-33-7Shld1Shield1Shield 1Shld 1Shld-1FKBPFK506-binding proteinhigh-affinity liganddestabilization domainHEK293NIH3T3Inhibitorinhibitorinhibit

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Shield-1 (Synonyms: Shld1)

Customer Review

Shield-1 Related Antibodies

10 Publications Citing Use of MCE Shield-1

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Biological Activity

Purity & Documentation

References

Customer Review

Shield-1 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Shield-1 Related Classifications

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