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SETDB1-TTD-IN-1

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Catalog No. T9742Cas No. 2755823-12-0

SETDB1-TTD-IN-1 is a potent and selective inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD, Kd = 88 nM), and also an endogenous binder competitive inhibitor with a KD of 0.106±0.002 μM for TTD. It can be used to study the biological functions and disease associations of SETDB1-TTD.

SETDB1-TTD-IN-1

SETDB1-TTD-IN-1

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Purity: 99.96%
Catalog No. T9742Cas No. 2755823-12-0
SETDB1-TTD-IN-1 is a potent and selective inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD, Kd = 88 nM), and also an endogenous binder competitive inhibitor with a KD of 0.106±0.002 μM for TTD. It can be used to study the biological functions and disease associations of SETDB1-TTD.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$269In StockIn Stock
5 mg$666In StockIn Stock
10 mg$948In StockIn Stock
25 mg$1,420In StockIn Stock
1 mL x 10 mM (in DMSO)$701In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.96%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
SETDB1-TTD-IN-1 is a potent and selective inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD, Kd = 88 nM), and also an endogenous binder competitive inhibitor with a KD of 0.106±0.002 μM for TTD. It can be used to study the biological functions and disease associations of SETDB1-TTD.
Targets&IC50
SETDB1-TTD:88 nM (Kd)
In vitro
METHODS: 16 additional tudor domains were expressed and purified from different tudor domain-containing proteins.
RESULTS SETDB1-TTD-IN-1 had Kd of 4.3 μM and 86 μM for 53BP1 and JMJD2A, respectively. SETDB1-TTD-IN-1 had no activity against 14 of the tudor domains (KD > 100 mM). [1]
METHODS: HEK293T cells stably transfected with pLVXmCherry-N1-SETDB1-TTD plasmid were treated with SETDB1-TTD-IN-1 (2.5, 5, 10, 20, 40 μM), and the protein content of the soluble part in the lysate was determined by western blot.
RESULTS SETDB1-TTD-IN-1 can effectively and dose-dependently stabilize SETDB1-TTD protein in HEK293T cells at a concentration of >= 5 μM.[1]
Chemical Properties
Molecular Weight469.58
FormulaC28H31N5O2
Cas No.2755823-12-0
SmilesCN1C[C@@H](C[C@@H](C1)c1ccc(OCc2ccccc2)cc1)Nc1nc2cc[nH]c2c(=O)n1CC=C
Relative Density.1.24 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 252.5 mg/mL (537.71 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.65 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
1mg5mg10mg50mg
1 mM2.1296 mL10.6478 mL21.2956 mL106.4781 mL
5 mM0.4259 mL2.1296 mL4.2591 mL21.2956 mL
10 mM0.2130 mL1.0648 mL2.1296 mL10.6478 mL
20 mM0.1065 mL0.5324 mL1.0648 mL5.3239 mL
50 mM0.0426 mL0.2130 mL0.4259 mL2.1296 mL
100 mM0.0213 mL0.1065 mL0.2130 mL1.0648 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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