DOT1

Isoform-selective Products

DOT1 Products

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  • DOT1 Inhibitors (3)
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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.
Exp Hematol Oncol, 2023, 12(1):81
EMBO Rep, 2023, e56233.
Life Sci Alliance, 2023, 6(5)e202201619
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 Rep, 2023, 42(8):112885
Cell Rep, 2023, 42(6):112566
Int J Mol Sci, 2023, 24(11)9365
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.
bioRxiv, 2024, 2024.02.06.579191
Cell Rep, 2023, 42(8):112885
Cell Rep, 2023, 42(6):112566
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.
Exp Hematol Oncol, 2023, 12(1):81
EMBO Rep, 2023, e56233.
Life Sci Alliance, 2023, 6(5)e202201619
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 Rep, 2023, 42(8):112885
Cell Rep, 2023, 42(6):112566
Int J Mol Sci, 2023, 24(11)9365
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.
bioRxiv, 2024, 2024.02.06.579191
Cell Rep, 2023, 42(8):112885
Cell Rep, 2023, 42(6):112566

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Tags: DOT1 inhibitor | DOT1 modulator | DOT1 Inhibition | DOT1 regulation