estrogen receptor modulator 1

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1 G0 phase, making it applicable in cancer research [1].

Estrogen receptor modulator11 (Compound 27) is a tetrahydroisoquinoline derivative. It exhibits affinity for the estrogen receptor (ER), with IC50 values of 285 nM for ERα and 421 nM for ERβ. Estrogen receptor modulator11 does not demonstrate antagonist activity in MCF-7 cell assays.

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

Toremifene (GTx 006) is a selective estrogen-receptor modulator (SERM).

(E Z)-Droloxifene is a mixture comprising (E)-Droloxifene, known as a selective estrogen receptor modulator, and (Z)-Droloxifene. (E)-Droloxifene binds to estrogen receptors (ER) in rabbit uterine homogenate with an IC50 of 24 nM. It increases uterine weight in immature rats and reduces the uterine weight increase caused by estradiol in juvenile rats. Additionally, (E)-Droloxifene inhibits the growth of human breast cancer cells MCF-7, ZR-75-1, and T47D stimulated by 17β-estradiol. In contrast, (Z)-Droloxifene shows weak binding to ER and exhibits neither estrogenic nor anti-estrogenic activity.

Levormeloxifene is a selective modulator of the estrogen receptor. It inhibits the production of vaginal tropoelastin and transforming growth factor-beta 1.

DK1 is a potent estrogen related receptor modulator. DK1 impacts the activity of ERRα receptor and reduces blood glucose. DK1 shows the potential in the diabetes research [1].

Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

ER degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (SERM) with the capacity to degrade Estrogen Receptor (ER)α. It disrupts the microtubule network, inhibits tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [1].

LY117018 TFA, an analog of Raloxifene, functions as a selective estrogen receptor modulator and demonstrates antiproliferative effects on breast cancer cell lines [1] [2] [3].