DOT1
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| 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 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 Ki 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. |
Western blot validation of H3K79me2 depletion in Jurkat cells. Mixtures of 0%–100% EPZ5676-treated cells (0:100; 25:75; 50:50, 75:25; 100:0 proportions of [DMSO-treated:EPZ5676-treated] cells) were measured by immunoblot (IB) for the presence of H3K79me2, H3K4me3, or total histone H3 (loading control). Treated cells were exposed to 20 μM EPZ5676 for 4 days.
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| S7079 |
SGC 0946SGC 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. |
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| S7353 |
EPZ004777EPZ004777 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. |
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. |
