Bioactivity | 6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting[1]. | ||||||||||||
Target | IC50: 21.5 μM (EYA3); metabolite | ||||||||||||
Invitro | 6-Hydroxybenzbromarone (7.5 μM; 72 hours) shows over 50% reduction in cell proliferation. Meanwhile, treatment with BBR and BZ also reduces cell viability, but none of the other compounds tested has a negative impact on cell viability or proliferation[1].6-Hydroxybenzbromarone (7.5 μM; 1-20 hours) has inhibitory affects EC migration tubulogenesis of HUVECs. However, the effect of 6OH-BBR on tube formation is attenuated in the presence of high concentrations of fetal bovine serum (FBS), likely reflecting non-specific protein binding[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
Name | 6-Hydroxybenzbromarone | ||||||||||||
CAS | 152831-00-0 | ||||||||||||
Formula | C17H12Br2O4 | ||||||||||||
Molar Mass | 440.08 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Pandey RN, et al. Structure-activity relationships of benzbromarone metabolites and derivatives as EYA inhibitory anti-angiogenic agents.PLoS One. 2013 Dec 18;8(12):e84582. |