DOT1
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| 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 |
- 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Ki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。 |
Treatment of c-Kit+ bone marrow (BM) cells from Setd2f/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.
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| S7079 |
SGC 0946SGC 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。 |
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| S7353 |
EPZ004777EPZ004777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。 |
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. |
