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> Shield-1 [914805-33-7]

Shield-1 [914805-33-7]

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Katalog-Nummer HY-112210-10mg

Size : 10mg

Marke : MedChemExpress


Beschreibung

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
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.

Shield-1 Related Antibodies

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.
Molekulargewicht

748.90

Formel

C42H56N2O10
CAS. Nr.
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
Versand

Shipping with dry ice.
Speicherung

-80°C, stored under nitrogen
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)

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
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.

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.
Reinheit & Dokumentation
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