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:88 nM (Kd)

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]