Taragarestrant (D-0502) is a potent, orally active estrogen receptor degrader. Taragarestrant has antiproliferative activity against estrogen receptor-positive breast cancer cell lines and has anticancer activity. Taragarestrant can be used for cancer research[1][2].
NNC45-0781 is a tissue-selective estrogen partial-agonist.
Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3].
GSK-4716 is a selective ERRβ/γ agonist.
Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1)[1].
Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors[1][2].
Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity[1][2].
ER degrader 3 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 3 has the potential for the research of cancer diseases (extracted from patent WO2018233591A1, compound 1)[1].
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[1].
Endoxifen Z-isomer 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). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.IC50 value: 1.6 μM [1]Target: hERG Potassium Channel, Estrogen Receptor/ERREndoxifen Z-isomer is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen Z-isomer observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen Z-isomer concentrations are needed when ERβ is absent.[2]
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 estrogen-related receptor alpha (ERRa) degrader[1].
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an >IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM)[1].
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC)[1][2].
Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7)[1].
Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity[1][2].
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380[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[1][2][3].
4',2-Dihydroxy-4,6-dimethoxydihydrochalcone, an estrogen agonist, shows binding affinity for bovine uterine estrogen receptor with an IC5050 of 15 μM[1].
Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing[1].
Enclomiphene ((E)-Clomiphene) hydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene hydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1].
Y134 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[1].