DOT1

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Catalog No. Product Name Information Product Use Citations Product Validations
S7062 Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Cancer Discov, 2022, candisc.0646.2021
Mol Cell, 2022, 82(6):1140-1155.e11
Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3
S7079 SGC 0946 SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Transpl Int, 2020, 33(2):229-243
Cancer Cell, 2019, 36(2):179-193
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6
S7062 Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Cancer Discov, 2022, candisc.0646.2021
Mol Cell, 2022, 82(6):1140-1155.e11
Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3
S7079 SGC 0946 SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Transpl Int, 2020, 33(2):229-243
Cancer Cell, 2019, 36(2):179-193
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.
Cell Res, 2022, 10.1038/s41422-022-00668-0
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6
Tags: DOT1 inhibitor | DOT1 modulator | DOT1 Inhibition | DOT1 regulation