dot1l in 1

The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.

Dot1L-IN-1 TFA is a potent and selective Dot1L inhibitor, with a K i of 2 pM and an IC50 of <0.1 nM. It effectively inhibits H3K79 dimethylation (IC50 = 3 nM) and suppresses HoxA9 promoter activity (IC50 = 17 nM) in HeLa and Molm-13 cells, respectively [1].

Dot1L-IN-8 (Compound 15) is an effective Dot1L inhibitor. It suppresses the viability of HL-60, K562, MV4-11, HH, and KG-1 cells, with IC50 values of 0.45, 1.03, 0.68, 1.66, and 1.12 μM, respectively.

S-N6-Methyladenosylhomocysteine (Chart 1-1) is a potent inhibitor of the histone methyltransferase DOT1L, with an IC50 of 0.29 μM. This compound plays a significant role in cancer research.

DOT1Lligand-1 is a ligand for DOT1L. It serves as a ligand for target proteins (Ligands for Target Protein for PROTAC) and is utilized in the synthesis of PROTACs targeting DOT1L, such as MS2133.

MS2133 is a DOT1L PROTAC degrader. It facilitates the ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells, with DC50 values of 56 nM and 25 nM, respectively, and reduces H3K79 methylation. MS2133 also inhibits the growth of MLL-r leukemia cells, demonstrating anticancer activity.

Dot1L-IN-7 (compound 25) is a selective and potent inhibitor of telomere silencing 1-like protein (DOT1L) with an IC50 of 1.0 μM. It selectively kills MLL-AF9 cells without affecting the growth of E2A-HLF cells.