Molecular Formula | C24H21N3O3 |
Molar Mass | 399.44 |
Solubility | DMSO: 10 mg/mL |
Appearance | powder |
Color | white to beige |
Storage Condition | 2-8°C |
Use | BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 µM. |
Target | G9a;PRC2 |
In vitro study | BRD9539 decreases ATP levels in a dose-dependent manner in HeLa cells. BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. However, BRD9539 has no activity in cell-based assays, presumably due to impaired cell permeability compared to that of BRD4770. In addition, the activities of 16 other chromatin-modifying enzymes and 100 kinases involved in cell-cycle regulation and cancer cell biology are tested for activity in the presence of 5 or 10 μM BRD9539; no activity is seen in any of these assays. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
Reference Show more | 1. Yuan, Y., Wang, Q., Paulk, J., et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma ACS Chem. Biol. 7(7), 1152-1157 (2012). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.503 ml | 12.517 ml | 25.035 ml |
5 mM | 0.501 ml | 2.503 ml | 5.007 ml |
10 mM | 0.25 ml | 1.252 ml | 2.503 ml |
5 mM | 0.05 ml | 0.25 ml | 0.501 ml |
biological activity | BRD9539 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μm. BRD9539 also inhibited PRC2 Activity and was inactive against SUV39H1,NSD2 and DNMT1. |