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SETDB1-TTD-IN-1 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 can be used for the research of biological functions and disease associations of SETDB1-TTD.

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

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