ERβ Antagonist
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Acolbifene
0 ImagesSynonyms: EM-652; SCH 57068Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.
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Y134
0 ImagesY134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.
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Estrogen receptor β antagonist 2
0 ImagesEstrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively.
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(R,R)-THC
0 Images(R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6.
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Acolbifene hydrochloride
0 ImagesSynonyms: EM-652 hydrochloride; SCH 57068 hydrochlorideAcolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
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ERα degrader 5
0 ImagesCat. No.: HY-146267CAS No.: 2941268-96-6ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
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Mansonone F
0 ImagesMansonone F acts as an estrogen receptor antagonist and an antimicrobial agent. Mansonone F effectively inhibits 17β-estradiol-induced β-galactosidase activity. Derivatives of Mansonone F also exhibit antioxidant and anti-Staphylococcus aureus biological activities. Mansonone F can be used in studies related to Staphylococcus aureus infections and methicillin-resistant Staphylococcus aureus (MRSA) infections.
