DOT1 inhibitor | DOT1 modulator | DOT1 Inhibition

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S7062	Pinometostat (EPZ5676)	<1 mg/mL	100 mg/mL	92 mg/mL
S7079	SGC 0946	<1 mg/mL	100 mg/mL	100 mg/mL
S7353	EPZ004777	<1 mg/mL	100 mg/mL	100 mg/mL

亜型選択性的な製品

DOT1L Selective

DOT1製品

All (3) DOT1阻害剤(3)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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 Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118 EMBO Rep, 2021, 22(2):e51184	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.	Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118 Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6 Cancer Cell, 2019, 35(5):752-766	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.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

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

Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118

EMBO Rep, 2021, 22(2):e51184

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.