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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

🥰Excellent
Purity: 99.38%
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 SizePriceAvailabilityQuantity
1 mg$269In Stock
5 mg$666In Stock
10 mg$948In Stock
25 mg$1,420In Stock
50 mg$1,890In Stock
100 mg$2,570In Stock
1 mL x 10 mM (in DMSO)$783In Stock
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Purity:99.38%
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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
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (95.83 mM)
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

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