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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $269 | In Stock | |
5 mg | $666 | In Stock | |
10 mg | $948 | In Stock | |
25 mg | $1,420 | In Stock | |
50 mg | $1,890 | In Stock | |
100 mg | $2,570 | In Stock | |
1 mL x 10 mM (in DMSO) | $783 | In Stock |
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] |
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 | Powder: -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
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