49 products were found matching "K11427"!

SGC0946 is an inhibitor of the non-SET domain-containing methyltransferase DOT1L (IC50 = 0.3 nM). It is selective for DOT1L over a panel of 12 additional protein methyltransferases, DNA methyltransferase 1 (DNMT1), and a panel of 29 receptors and ion channels. SGC0946 reduces the levels of dimethylated lysine 79 on...

Description: Histone-lysine N-methyltransferase, H3 lysine-79 specific, also known as Histone H3-K79 methyltransferase, DOT1-like protein, Lysine N-methyltransferase 4 and DOT1L, is a nucleus protein which belongs to theDOT1 family. In contrast to other lysine histone methyltransferase, DOT1L does not contain a SET...

Description: 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. Target: Histone Methyltransferase. Smiles:...

Description: SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM), selectively kill mixed lineage leukemia cells. Target: Histone Methyltransferase. Smiles: CC(C)N(CCCNC(=O)Nc1ccc(cc1)C(C)(C)C)C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(Br)c2c(N)ncnc12. References: Yu W, et al. Nat...

DOT1L is a non-SET domain containing methyltransferase whose function is important for the transcriptional activation of certain genes, DNA damage repair, and cell cycle regulation. DOT1L is known to play an essential role in MLL-rearranged leukemias, and thus has emerged as a drug target for these leukemias....

DOT1L is a protein methyltransferase (PMT). It is the only enzyme known to methylate histone 3 at lysine 79 (H3K79), where it catalyzes mono-, di-, and trimethylation. Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation. SGC0946 is a potent...

EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model. It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases. DOT1L inhibition by EPZ004777 has also...

Protein function: Histone methyltransferase. Methylates 'Lys-79' of histone H3. Nucleosomes are preferred as substrate compared to free histones. Binds to DNA. [The UniProt Consortium]

Protein function: Histone methyltransferase. Methylates 'Lys-79' of histone H3. Nucleosomes are preferred as substrate compared to free histones. Binds to DNA. [The UniProt Consortium]

EPZ-5676 is an inhibitor of DOT1L histone methyltransferase (HMT) that exhibits anticancer chemotherapeutic activity. In acute myelogenous leukemia (AML) cells with MLL gene translocations, EPZ-5676 displays cytotoxicity, in similar animal models, this compound induces tumor regression without toxicity.

EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 400 pM. EPZ004777 selectively kills a variety of MLL-rearranged leukemia cells, including an MLL-AF4 leukemia cell line MV4-11 and an MLL-AF9 leukemia cell line MOLM13.

The DOT1L Chemiluminescent Assay Kit is designed to measure DOT1L activity for screening and profiling applications. The key to the DOT1L Chemiluminescent Assay Kit is a highly specific antibody that recognizes methylated K79 residue of H3. With this kit, only three simple steps on a microtiter plate are required...