| Bioactivity | LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells[1]. | ||||||||||||
| Target | Kd: 99 nM (BRD9) | ||||||||||||
| Invitro | LP99 disrupts BRD9 interactions with chromatin at a concentration of 0.8 μM. BRD7- and BRD9-NanoLuc luciferase fusion proteins and fluorescently labelled histone H3.3- and H4-HaloTag fusions were expressed in HEK293 cells. The addition of LP99 decreased BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose-dependent manner, with cellular IC50 values in the low micromolar range for both histone. Cytotoxicity tests in U2OS cells for 24 and 72 hours shows the inhibitor to be non-toxic at concentrations of <33 μM. LP99 inhibits IL-6 secretion from THP-1 cells in a dose-dependent manner[1]. | ||||||||||||
| Name | LP99 | ||||||||||||
| CAS | 1808951-93-0 | ||||||||||||
| Formula | C26H30ClN3O4S | ||||||||||||
| Molar Mass | 516.05 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Clark PG, et al. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. |