Estrogen Receptor/ERR

PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

(±)-Medicarpin, a pterocarpan, is a type of isoflavonoid isolated from several medicinal plant species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum, Platymiscium floribundum, and so on. (±)-Medicarpin potently inhibits osteoclastogenesis and promotes bone healing and increases bone mass by osteoblast differentiation with estrogen receptor (ER) β-mediated osteogenic action.

(20S)-Protopanaxatriol is a metabolite derived from ginsenosides, possessing diverse biological activities and pharmacological effects.

(E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.

AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property.

Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer drug substance. Endoxifen E-isomer exhibits antiestrogenic effects.

Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer drug substance. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects.

Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.

Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).

ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).

GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist.

PROTAC ERRalpha Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.

PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.

SNIPER(ER)-110 consists of a IAP ligand and an estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively.

A hepatic metabolite of zearalenone

Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.

PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.

ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.

N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.