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Shield-1 [914805-33-7]

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Référence NB-64-05447-10mg

Conditionnement : 10mg

Marque : Neo Biotech

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Shield-1

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Catalog No. T13884 Copy Product Info

Purity: 99.45%

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Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.

Cas No. 914805-33-7

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.45%

Color:White

Product Information

Shield-1 AI Summary

Shield-1 displays a strong binding affinity to various FKBP12 mutants. It binds to the human FKBP F36V mutant with a Kd of 2.4 nM and the human FKBP F36V/L106P mutant-YFP fusion protein in NIH3T3 cells after 24 hours, with an EC50 of 100.0 nM. It stabilizes the FKBP12 V2A mutant-YFP fusion protein with an EC50 of 60.0 nM and displaces fluorescein-SLF from the FKBP12 F36V mutant with a Kd of 0.4 nM. Additionally, it displaces fluorescein-SLF from FKBP12 mutants F36V, V2A, L50A, L106A with Kd values ranging from 2.0 to 4.0 nM. Moreover, microarray analysis in mouse NIH3T3 cells indicates that Shield-1 induces gene expression changes, positively affecting mRNA levels of Epb4.1l2, Csnkle, and Tcfe3 (FC 1.9 to 2.7) and negatively affecting MtCrVgp3, 4930422M22Rik, A430110N23, Ptpn1, Npas4, and Shkbp1 (FC -1.7 to -11.3). These findings suggest that Shield-1 has significant bioactivity and can modulate various cellular processes and pathways..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.
Targets & IC50	FKBP12 V2A mutant-YFP fusion protein (NIH3T3 cells):100 nM (EC50), FKBP12 V2A mutant-YFP fusion protein (NIH3T3 cells):60 nM
In vitro	Method: Transfected cells with mtFKBP-TRPV5 were treated with Shield-1 (1 μM, 24 hours), the ligand was washed out, and the mtFKBP-TRPV5 signal was subsequently measured at different time points. Result mtFKBP-TRPV5 protein levels decreased rapidly with a half-life (t) of 2.53 ± 0.59 hours. ^[1]

Chemical Properties

Molecular Weight	748.9
Formula	C₄₂H₅₆N₂O₁₀
Cas No.	914805-33-7
Smiles	CC[C@H](C(=O)N1CCCC[C@H]1C(=O)O[C@H](CCc1ccc(OC)c(OC)c1)c1cccc(OCCN2CCOCC2)c1)c1cc(OC)c(OC)c(OC)c1
Relative Density.	1.168 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store under nitrogen, Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (333.82 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (6.68 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.3353 mL	6.6765 mL	13.3529 mL	66.7646 mL
5 mM	0.2671 mL	1.3353 mL	2.6706 mL	13.3529 mL
10 mM	0.1335 mL	0.6676 mL	1.3353 mL	6.6765 mL
20 mM	0.0668 mL	0.3338 mL	0.6676 mL	3.3382 mL
50 mM	0.0267 mL	0.1335 mL	0.2671 mL	1.3353 mL
100 mM	0.0134 mL	0.0668 mL	0.1335 mL	0.6676 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

Shld-1Shld1Shld 1Shield-1Shield1Shield 1NIH3T3Inhibitorinhibithigh-affinity ligandHEK293FKBPFK506-binding proteindestabilization domain

Related Tags: Shield-1 chemical structure | Shield-1 in vitro | Shield-1 formula | Shield-1 molecular weight