DOT1

抑制剂选择性比较

DOT1产品

所有产品(3) DOT1抑制剂(3)

目录号	产品描述	文献引用	实验数据
S7062	Pinometostat (EPZ5676) Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂，无细胞试验中K_i为80 pM，比作用于所有其他测试的PMTs选择性高37000倍以上，抑制肿瘤中H3K79甲基化。Phase 1。	Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3 Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9 Bone, 2021, 142:115677	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是一种高效的，选择性的DOT1L甲基转移酶抑制剂，无细胞试验中IC50为0.3 nM，对一系列12 PMTs和DNMT1没有活性。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Sci Adv, 2019, 5(2):eaav5590
S7353	EPZ004777 EPZ004777是一种有效的，选择性的DOT1L抑制剂，无细胞试验中IC50为0.4 nM。	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.

目录号

产品描述

文献引用

实验数据

S7062

Pinometostat (EPZ5676)

Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂，无细胞试验中K_i为80 pM，比作用于所有其他测试的PMTs选择性高37000倍以上，抑制肿瘤中H3K79甲基化。Phase 1。

Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3

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

Bone, 2021, 142:115677

S7079

SGC 0946

SGC 0946是一种高效的，选择性的DOT1L甲基转移酶抑制剂，无细胞试验中IC50为0.3 nM，对一系列12 PMTs和DNMT1没有活性。

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

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

Sci Adv, 2019, 5(2):eaav5590

S7353

EPZ004777

EPZ004777是一种有效的，选择性的DOT1L抑制剂，无细胞试验中IC50为0.4 nM。

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

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

Sci Adv, 2019, 5(2):eaav5590

目录号	产品描述	文献引用	实验数据
S7062	Pinometostat (EPZ5676) Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂，无细胞试验中K_i为80 pM，比作用于所有其他测试的PMTs选择性高37000倍以上，抑制肿瘤中H3K79甲基化。Phase 1。	Nat Biotechnol,2021, 10.1038/s41587-021-00837-3 Cell Mol Gastroenterol Hepatol,2021, S2352-345X(21)00019-9 Bone,2021, 142:115677	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是一种高效的，选择性的DOT1L甲基转移酶抑制剂，无细胞试验中IC50为0.3 nM，对一系列12 PMTs和DNMT1没有活性。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Sci Adv,2019, 5(2):eaav5590
S7353	EPZ004777 EPZ004777是一种有效的，选择性的DOT1L抑制剂，无细胞试验中IC50为0.4 nM。	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.

目录号

产品描述

文献引用

实验数据

S7062