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DOT1

Isoform-selective Products

DOT1 Products

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  • DOT1 Inhibitors (4)
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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.
Cell Biosci, 2024, 14(1):93
Int J Mol Sci, 2024, 25(11)6020
Heliyon, 2024, 10(13):e33736
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.
Nat Commun, 2024, 15(1):10787
Life Sci Alliance, 2024, 7(4)e202302424
Sci Adv, 2024, 10(38):eadn7724
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.
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.
Cell Biosci, 2024, 14(1):93
Int J Mol Sci, 2024, 25(11)6020
Heliyon, 2024, 10(13):e33736
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.
Nat Commun, 2024, 15(1):10787
Life Sci Alliance, 2024, 7(4)e202302424
Sci Adv, 2024, 10(38):eadn7724
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.
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.

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