Catalog No.
Product Name
Application
Product Information
Citations
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ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- Asmaa R. Abdel-Hamed, .et al. , J Med Chem Sci, 2023, 6: 250-268
- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
- Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
- Ewa Domarecka, .et al. , Brain Sci, 2025, Apr 24;15(5):441 PMID: 40426612
- Shuang Liang, .et al. , Cardiovasc Ther, 2022, Apr 7;2022:7145699 PMID: 35474714
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Estrogen receptor agonist
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.- Gao X, .et al. , Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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GPR119 agonist
GSK-1292263 is a novel GPR119 agonist.- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
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Progesterone/ERR Agonist
Etonogestrel is a steroidal progestin used in hormonal contraceptives, most notably the subdermal implant Nexplanon and the vaginal ring NuvaRing.- Linying Li, .et al. , Pharmaceuticals (Basel), 2022, Oct 3;15(10):1226 PMID: 36297338
- Linying Li, .et al. , J Control Release, 2021, Dec 10;340:188-199 PMID: 34678316
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Estrogen receptor antagonist
Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.- Marina Arino Martin, .et al. , Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. , Water Res, 2019, Dec 29;171:115451 PMID: 31901682
- Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
- Muthulakshmi S, .et al. , J Appl Toxicol, 2018, Nov;38(11):1388-1397 PMID: 29923290
- Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene acetate significantly prevents bone mass loss at 20 mg/day in healthy postmenopausal women with normal or low bone mineral density.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
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Estrogen receptor antagonist
Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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ERRβ & ERRγ Agonist
GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.- Shike Zhang, .et al. , Journal of Environmental Sciences, 2024, Oct, 8 PMID: 40412923
- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
- Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
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estrogen receptor modulator
acolbifene is a substance being studied in the prevention of breast cancer in women at high risk of breast cancer. Acolbifene hydrochloride binds to estrogen receptors in the body and blocks the effects of estrogen in the breast. It is a type of selective estrogen receptor modulator (SERM).- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
- Lirit N. Franks, .et al. , Front Pharmacol, 2016, 7: 503 PMID: 28066250
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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Estrogen receptor antagonist
(E/Z)-4-hydroxy Tamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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ERα agonist
Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist. -
estrogen agonist
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist. - Liquiritigenin is a plant-derived highly selective estrogen receptor ?? agonist
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Estrogen receptor degrader
Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. -
estrogen receptor modulator
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM). -
Estrogen receptor degrader
Brilanestrant (GDC-0810, ARN-810??? is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors. -
SERD/SERM
RAD1901 is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. - Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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ER antagonist
Fulvestrant S enantiomer is the S enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer. -
estrogen receptor modulator
4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM). -
ERbeta agonist
Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta. -
estrogen receptor degrader
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases. -
estrogen ligand
Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER. -
Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
ERRβ agonist
WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM. - (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
- 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).
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EStrogen receptor (ER) antagonist
GW7604 is an antiestrogen agbent, and is tthe presumed metabolite of GW5638 in breast (MCF-7) and endometrial (ECC-1) cell lines in vitro. -
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.
