DOT1 inhibitor | DOT1 modulator | DOT1 Inhibition

Inhibitory Selectivity

Isoform-specific Inhibitors

DOT1L Selective

DOT1 Products

All (3) DOT1 Inhibitors (3)

Catalog No.	Information	Product Use Citations	Product Validations
S7062	Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i 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 Biotechnol, 2021, 10.1038/s41587-021-00837-3 EMBO Rep, 2021, 22(2):e51184 Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9	Treatment of c-Kit+ bone marrow (BM) cells from Setd2^f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400 nM for 24 h. Then cells were collected to determine the proteins levels of RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.
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.	Transpl Int, 2020, 33(2):229-243 Cancer Cell, 2019, 36(2):179-193 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.	Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6 Cancer Cell, 2019, 35(5):752-766 Sci Adv, 2019, 5(2):eaav5590	THP-1 cells were treated with MI-3 (6.25 μM, 6 days), GSK126 (5 μM, 6 days), or EPZ004777 (5 μM, 6 days), with orwithout PMA (50 ng/mL, 12 h), and surface expression of CD11b was determined by ﬂow cytometric analysis. The data are representedas the mean ± SD, n = 3. THP-1 cells were collected for Wright-Giemsa staining.

Catalog No.

Information

Product Use Citations

Product Validations

S7062

Pinometostat (EPZ5676)

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i 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 Biotechnol, 2021, 10.1038/s41587-021-00837-3

EMBO Rep, 2021, 22(2):e51184

Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9

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.

Transpl Int, 2020, 33(2):229-243

Cancer Cell, 2019, 36(2):179-193

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.

Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6

Cancer Cell, 2019, 35(5):752-766

Sci Adv, 2019, 5(2):eaav5590

Catalog No.	Information	Product Use Citations	Product Validations
S7062	Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i 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 Biotechnol, 2021, 10.1038/s41587-021-00837-3 EMBO Rep, 2021, 22(2):e51184 Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9	Treatment of c-Kit+ bone marrow (BM) cells from Setd2^f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400 nM for 24 h. Then cells were collected to determine the proteins levels of RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.
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.	Transpl Int, 2020, 33(2):229-243 Cancer Cell, 2019, 36(2):179-193 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.	Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6 Cancer Cell, 2019, 35(5):752-766 Sci Adv, 2019, 5(2):eaav5590	THP-1 cells were treated with MI-3 (6.25 μM, 6 days), GSK126 (5 μM, 6 days), or EPZ004777 (5 μM, 6 days), with orwithout PMA (50 ng/mL, 12 h), and surface expression of CD11b was determined by ﬂow cytometric analysis. The data are representedas the mean ± SD, n = 3. THP-1 cells were collected for Wright-Giemsa staining.