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  2. FKBP
  3. Shield-1

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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CAS 番号 : 914805-33-7

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 741 在庫あり
Solution
10 mM * 1 mL in DMSO USD 741 在庫あり
Solid
1 mg $200 在庫あり
5 mg $450 在庫あり
10 mg $730 在庫あり
25 mg $1200 在庫あり
50 mg $1600 在庫あり
100 mg $2150 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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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    製品説明

    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].

    IC50 & Target

    FKBP12

     

    Cellular Effect
    Cell Line Type Value Description References
    NIH3T3 EC50
    60 1
    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]
    NIH3T3 EC50
    100 1
    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
    100 1
    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
    100 1
    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 1
    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]
    NIH3T3 EC50
    60 1
    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]
    体外実験

    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.
    分子量

    748.90

    分子式

    C42H56N2O10

    CAS 番号
    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

    輸送条件

    Shipping with dry ice.

    保管条件

    -80°C, stored under nitrogen

    溶剤 & 溶解度
    体外: 

    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)

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

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    体内:

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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.
    純度とドキュメンテーション

    純度: 99.73%

    参考文献

    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
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    • Molarity Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
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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.

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    Inquiry Information

    製品名:
    Shield-1
    製品番号:
    HY-112210
    数量:
    MCE 日本正規代理店: