| Name | SETDB1-TTD-IN-1 |
| 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. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.65 mM), Sonication is recommended. DMSO : 252.5 mg/mL (537.71 mM), Sonication is recommended.
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| Keywords | SETDB1-TTD-IN-1 | SETDB-1-TTD-IN-1 | SETDB1TTDIN1 | SETDB1-TTD | SETDB1 TTD IN 1 | HistoneMethyltransferase | Histone Methyltransferase |
| Inhibitors Related | MAK-683 hydrochloride | SNDX-5613 | Tazemetostat | Piribedil | XY1 | UNC 0631 | (Iso)-Flavokawain A | EPZ015666 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | High-Efficiency Gene Editing Small Molecule Library |