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DOT1

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Isoform-selective Products

Cat.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.
Nat Commun, 2025, 16(1):10324
Blood Adv, 2025, bloodadvances.2024015427
J Neurotrauma, 2025, 10.1177/08977151251374286
Verified customer review of Pinometostat (EPZ5676)
E8279New SPA-10091-HCl SPA-10091-HCl is a degrader of DOT1L that selectively degrades DOT1L protein through the nuclear ubiquitin-proteasome pathway, thereby suppressing H3K79 methylation in CRPC cells. It also inhibits DOT1L enzymatic activity with an IC50 of 0.87 μM, induces apoptosis, and significantly reduces tumor growth in vivo.
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.
NPJ Regen Med, 2024, 9(1):42
Cell Rep, 2023, 42(8):112885
Cell Rep, 2023, 42(6):112566
Verified customer review of EPZ004777
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, and is inactive against a panel of 12 PMTs and DNMT1.
Nat Commun, 2024, 15(1):10787
NPJ Regen Med, 2024, 9(1):42
Life Sci Alliance, 2024, 7(4)e202302424