SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a K_d of 88 nM. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD.

SETDB1-TTD-IN-1 TFA shows some activity for 53BP1 and JMJD2A, with K_ds of 4.3 μM and 86 μM, respectively. SETDB1-TTD-IN-1 TFA does not show activity against 14 of the 16 tested tudor domains (K_d>100 μM).
SETDB1-TTD-IN-1 (2.5-40 μM) TFA efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells.
SETDB1-TTD-IN-1 (2.5-40 μM; 24 h) TFA significantly affected the expression of 72 genes in human acute monocytic leukemia THP-1 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Guo Y, et, al. Structure-Guided Discovery of a Potent and Selective Cell-Active Inhibitor of SETDB1 Tudor Domain. Angew Chem Int Ed Engl. 2021 Apr 12;60(16):8760-8765.  [Content Brief]