Estrogen Receptor/ERR Inhibitor

Estrogen Receptor/ERR Inhibitors (105):

Cat. No.	Product Name	Effect	Purity

HY-41570

3-Formylsalicylic acid	Inhibitor	98.06%
3-Formylsalicylic acid is a noncompetitive estrone sulfatase inhibitor with an IC₅₀ value of 0.15 mM, a K_i value of 0.12 mM. 3-Formylsalicylic acid shows a low acute toxicity.

HY-14590

Kaempferol	Inhibitor	99.92%
Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.

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-14589

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

HY-136255

Camizestrant	Inhibitor	99.32%
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-111226

GSK5182	Inhibitor	99.10%
GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC₅₀ of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).

HY-19822A

Elacestrant dihydrochloride	Inhibitor	99.54%
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-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-15449

Kaempferide	Inhibitor	99.80%
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-B1100

Estradiol cypionate	Inhibitor	99.47%
Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.

HY-12864

Brilanestrant	Inhibitor	99.85%
Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC₅₀ of 0.7 nM.

HY-129079

TFMB-(R)-2-HG	Inhibitor	98.26%
TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG and acute myeloid leukemia (AML) oncogenic factor. TFMB-(R)-2-HG competitively inhibits α-ketoglutarate-dependent dioxygenases such as KDM2B and FTO. TFMB-(R)-2-HG impairs cell differentiation in response to Estrogen withdrawal. TFMB-(R)-2-HG is used in acute myeloid leukemia and glioma research.

HY-101447A

SI-2 hydrochloride	Inhibitor	98.06%
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.

HY-128600

ERD-308	Inhibitor	99.05%
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC₅₀ values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker：(HY-172645))

HY-18719B

Endoxifen hydrochloride	Inhibitor	98.04%
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.

HY-101405

Gestrinone	Inhibitor	99.76%
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-18719

Endoxifen (Z-isomer)	Inhibitor	99.20%
Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) 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-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-119437

FLTX1	Inhibitor	99.75%
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.

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