SETDB1-TTD-IN-1 TFA 

SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a K_d of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD^[1][2].

SETDB1-TTD-IN-1 (compound (R,R)-59) 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)^[1].
SETDB1-TTD-IN-1 (2.5-40 μM) TFA efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

583.60

C₃₀H₃₂F₃N₅O₄

Solid

White to off-white

CN1C[C@@H](C2=CC=C(OCC3=CC=CC=C3)C=C2)C[C@@H](NC4=NC5=C(C(N4CC=C)=O)NC=C5)C1.OC(C(F)(F)F)=O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [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.  [Content Brief]

  [2]. Uguen M, et, al. SETDB1 Triple Tudor Domain Ligand, (R, R)-59, Promotes Methylation of Akt1 in Cells. ACS Chem Biol. 2023 Aug 18;18(8):1846-1853.  [Content Brief]