Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

SETDB1-TTD-IN-1 [2755823-12-0]

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Referentie T9742-1mg

Formaat : 1mg

Merk : TargetMol

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SETDB1-TTD-IN-1

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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.

Cas No. 2755823-12-0

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

Batch Information

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Purity:99.96%

Appearance:Solid

Color:White

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COA HNMR LCMS

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 Weight	469.58
Formula	C₂₈H₃₁N₅O₂
Cas No.	2755823-12-0
Smiles	CN1C[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

Storage

Keep away from direct sunlight,Store under nitrogen, Powder: -20°C for 3 years | In 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

	1mg	5mg	10mg	50mg
1 mM	2.1296 mL	10.6478 mL	21.2956 mL	106.4781 mL
5 mM	0.4259 mL	2.1296 mL	4.2591 mL	21.2956 mL
10 mM	0.2130 mL	1.0648 mL	2.1296 mL	10.6478 mL
20 mM	0.1065 mL	0.5324 mL	1.0648 mL	5.3239 mL
50 mM	0.0426 mL	0.2130 mL	0.4259 mL	2.1296 mL
100 mM	0.0213 mL	0.1065 mL	0.2130 mL	1.0648 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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