dot1l

Dot1L-IN-9 (Compound 12) is a DOT1L inhibitor with an IC50 of 125 nM. It effectively reduces H3K79 dimethylation and is utilized in leukemia research.

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

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.

Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively.

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-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.

MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L (IC50 = 2 nM), a key epigenetic regulatory protein involved in the development of cancers such as hematologic malignancies, thus MU1656 was able to significantly inhibit the proliferation of cancer cells and induce apoptosis.

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor (Ki=80 pM). Pinometostat has antitumor activity and can be used in experiments to study a variety of leukemia treatments.

EPZ004777 is a potent and selective DOT1L inhibitor with an IC50 of 0.4 nM.

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

EPZ004777 hydrochloride (EPZ004777 HCl) is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

EPZ-4777 acts as a selective DOT1L inhibitor, effectively blocking the expression of leukemia-inducing genes by inhibiting methylation of H3K79 in cancer cells, and selectively targets and eradicates cells carrying translocations of this gene. It is utilized in tumor research.

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.

CN-SAH is a potent and selective inhibitor of DOT1L.