4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)-

Biological Activity

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 Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD[1]. SETDB1-TTD-IN-1 shows some activity for 53BP1 and JMJD2A, with Kds of 4.3 μM and 86 μM, respectively. SETDB1-TTD-IN-1 does not show activity against 14 of the 16 tested tudor domains (Kd>100 μM)[1].SETDB1-TTD-IN-1 (2.5-40 μM) efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells[1].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[1].

References

[1]. 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.