Estrogen Receptor/ERR Inhibitor

Estrogen Receptor/ERR Inhibitors (75):

Cat. No.	Product Name	Effect	Purity

HY-138642

Vepdegestrant	Inhibitor	99.60%
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC₅₀) of about 2 nM.

HY-19822

Elacestrant	Inhibitor	99.80%
Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC₅₀s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER⁺ breast cancer cell lines in vitro and in vivo.

HY-164764

ADX61623	Inhibitor	98.84%
ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease.

HY-14589

Chrysin	Inhibitor	99.85%
Chrysin is one of the most well known estrogen blockers.

HY-136255

Camizestrant	Inhibitor	98.04%
Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER⁺ HER2-advanced breast cancer.

HY-19822A

Elacestrant dihydrochloride	Inhibitor	99.72%
Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC₅₀s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER⁺ breast cancer cell lines in vitro and in vivo.

HY-15449

Kaempferide	Inhibitor	99.35%
Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.

HY-N2335

Coumestrol	Inhibitor	98.28%
Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC₅₀ of 50 μM.

HY-B1100

Estradiol cypionate	Inhibitor	99.62%
Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.

HY-12864

Brilanestrant	Inhibitor	99.95%
Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC₅₀ of 0.7 nM.

HY-128600

ERD-308	Inhibitor	99.17%
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).

HY-101447A

SI-2 hydrochloride	Inhibitor	99.79%
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC₅₀ values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.

HY-112100

PROTAC ERα Degrader-5	Inhibitor	98.96%
PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

HY-12825

BHPI	Inhibitor	≥98.0%
BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.

HY-18719

Endoxifen (Z-isomer)	Inhibitor	99.20%
Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.

HY-101405

Gestrinone	Inhibitor	99.69%
Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC₅₀ of 43.67 μM. Gestrinone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-18719A

Endoxifen Z-isomer hydrochloride	Inhibitor	99.67%
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).

HY-N6710

α-Zearalenol	Inhibitor	99.63%
α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.

HY-N1507

Tracheloside	Inhibitor	99.77%
Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.

HY-112098

PROTAC ERα Degrader-1	Inhibitor
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.

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