DOT1L Inhibitor

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

EPZ004777 is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 can be used for the study of leukemia.

SGC0946 is a selective DOT1L inhibitor with an IC₅₀ value of 0.3 nM. By inhibiting DOT1L, SGC0946 can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 can be used in the research of tumors such as leukemia and breast cancer, and also serves as a probe to further investigate the cellular mechanisms of DOT1L in normal and diseased cells.

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC_{50 SPA DOT1L} of 0.11 nM.

EPZ004777 hydrochloride is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 hydrochloride reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 hydrochloride selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 hydrochloride can be used for the study of leukemia.

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC₅₀ of 0.17 nM.

DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC₅₀ value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity.

Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a K_i of 2 pM and an IC₅₀ of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC₅₀=3 nM), as well as the activity of the HoxA9 promoter (IC₅₀=17 nM) in HeLa and Molm-13 cells, respectively.

Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a K_i of 2 pM and an IC₅₀ of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC₅₀=3 nM), as well as the activity of the HoxA9 promoter (IC₅₀=17 nM) in HeLa and Molm-13 cells, respectively.

Dot1L-IN-9 (Compound 12) is a DOT1L inhibitor (IC₅₀: 125 nM). Dot1L-IN-9 reduces H3K79 dimethylation. Dot1L-IN-9 can be used for anti-leukemia research.

MS2734 is a dual-substrate NNMT inhibitor that acts as a SAM (HY-B0617) competitor and a non-competitor of Nicotinamide (HY-B0150), with an IC₅₀ of 14 μM and a K_d of 2.7 μM against hNNMT. MS2734 inhibits the methyltransferase activities of DOT1L (IC₅₀ 1.3 μM), PRMT7 (IC₅₀ 20 μM), BCDIN3D (IC₅₀ 40 μM) and SMYD2 (IC₅₀ 62 μM). MS2734 is applicable to research related to diabetes, obesity and various cancers.

SGC0946 TFA is a selective DOT1L inhibitor with an IC₅₀ value of 0.3 nM. By inhibiting DOT1L, SGC0946 TFA can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 TFA can be used in the research of tumors such as leukemia and breast cancer, and also serves as a probe to further investigate the cellular mechanisms of DOT1L in normal and diseased cells.

Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells.

EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.

MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L, with an IC₅₀ of 2 nM. MU1656 can be used for the research of hematological malignancies.