DOT1

所有产品 DOT1抑制剂(3)

产品目录	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。	Haematologica, 2018, 103(7):1110-1123 Theranostics, 2018, 8(16):4359-4371 Cell Mol Immunol, 2018, 10.1038/s41423-018-0170-4	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。
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。	Theranostics, 2018, 8(16):4359-4371 Bioorg Med Chem, 2018, 26(8):1751-1758 Int J Cancer, 2017, 141(2):324-335	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.

产品目录

产品描述

文献引用

实验数据

S7062

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。

S7079

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。

S7353

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。

产品目录	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。	Haematologica,2018, 103(7):1110-1123 Theranostics,2018, 8(16):4359-4371 Cell Mol Immunol,2018, 10.1038/s41423-018-0170-4	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。
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。	Theranostics,2018, 8(16):4359-4371 Bioorg Med Chem,2018, 26(8):1751-1758 Int J Cancer,2017, 141(2):324-335	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.

产品目录

产品描述

文献引用

实验数据

S7062