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Estrogenreceptorα antagonist 1 (compound 35) is a highly selective antagonist of estrogenreceptorα, with IC50s of 0.02, 6.55 and 7.73 μM for estrogenreceptorα, estrogenreceptor β and MCF-7 cells, respectively. Estrogenreceptorα antagonist 1 can be used for the research of cancer .
Desketoraloxifene is an estrogenreceptorsalpha(ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogenreceptoralpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer .
Estrogenreceptor antagonist 1 is a selective estrogenreceptor antagonist. Estrogen (E2) and estrogenalphareceptor (ERα) are important drivers of breast cancer development. Estrogenreceptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .
Estrogenreceptor antagonist 2 is a selective estrogenreceptor downregulator. Estrogen (E2) and estrogenalphareceptor (ERα) are important drivers of breast cancer development. Estrogenreceptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .
Ospemifene is a non-estrogen selective estrogenreceptor modulator (SERM), with Kis of 380 and 410 nM for estrogenreceptorα (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptoralpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptoralpha (ERRa) degrader .
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptoralpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptoralpha (ERRa) degrader .
Propyl pyrazole triol (PPT) is a selective estrogenreceptoralpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogenreceptor beta (ERβ: 0.12%) .
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 estrogenreceptor-alpha (ERα).
CMP8, a selective ligand for estrogenreceptor, binds to the mutant estrogenreceptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively .
Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogenreceptoralpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle .
(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptoralpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptoralpha (ERRa) degrader .
GNE-149 is an orally bioavailable full antagonist of estrogenreceptorα (ERα; IC50=0.053 nM). GNE-149 is a selective estrogenreceptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
Estrogenreceptor modulator 8 (compound 4) is an orally active inhibitor of EstrogenReceptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogenreceptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
Estrogenreceptor β antagonist 2 is a potent and selective estrogenreceptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively .
Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogenreceptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogenreceptorα (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects[1][2].
Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogenreceptorα (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER .
MPP is a highly selective estrogenreceptoralpha (ERα) antagonist. MPP reduces the ratio of p-ERα/ERα .
https://www.ncbi.nlm.nih.gov/pubmed/29799481
Labouesse MA, et al. Effects of selective estrogenreceptoralpha and beta modulators on prepulse inhibition in male mice. Psychopharmacology (Berl). 2015 Aug;232(16):2981-94.
https://www.ncbi.nlm.nih.gov/pubmed/25893642
TPBM is a potent estrogenreceptorα (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
AZD9496 is a potent and selective estrogenreceptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD).
AZD9496 maleate is a potent and selective estrogenreceptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
Ferutinin, a natural terpenoid compound, is an estrogenreceptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca 2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities .
α-Zearalenol is a Mycotoxin with high affinity for the estrogenreceptors (ER),
α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects .
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogenreceptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .
Vepdegestrant (ARV-471) is an orally active PROTACestrogenreceptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogenreceptoralpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogenreceptors 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 .
DK1 is a potent modulator of estrogen related receptor. DK1 has an ability in reducing blood glucose, and impacts the activity of ERRαreceptor. DK1 has the potential for the research of diabetes .
G-36 is a cell permeable non-steroidal antagonist of G-protein-coupled estrogenreceptor (GPER/GPR30) which selectively inhibits estrogen-mediated activation of PI3K by GPER, but not by ERα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM) .
(±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogenreceptor modulator (SERM) (EstrogenReceptor/ERR) that inhibits ERα and ERβ with IC50s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research .
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogenreceptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
α-Zearalenol (Standard) is the analytical standard of α-Zearalenol. This product is intended for research and analytical applications. α-Zearalenol is a Mycotoxin with high affinity for the estrogenreceptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects .
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogenreceptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
Isocurcumenol, an estrogenreceptoralpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively .
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 estrogenreceptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
PROTAC ERRα ligand 2 is an estrogen-related receptorα (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) .
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 estrogenreceptor-alpha (ERα) degrader.
Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogenreceptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .
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) .
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptorα) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research .
Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogenreceptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
(20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogenreceptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects .
PROTAC ERα Degrader-7 (compound i-320) is a potent estrogenreceptoralpha(ERα) PROTAC degrader with a DC50 value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring .
Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogenreceptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively .
WAY-204688 is an estrogenreceptor(ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptoralpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader .
DS45500853 is an estrogen-related receptorα (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) .
DS20362725 is an estrogen-related receptorα (ERRα) agonist. DS20362725 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 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogenreceptorα. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6 .
Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogenreceptorα. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6 .
PROTAC ERα Degrader-2 comprises a IAP ligand binding group, a linker and an estrogenreceptorα (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
ERα degrader-2 is a selective estrogenreceptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER + breast cancer research .
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogenreceptor-alpha (ERα) Y537S degrader .
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptorα (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 .
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogenreceptors ERα and ERβ .
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 estrogenreceptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
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 estrogenreceptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
ER degrader 6 (compound 35s) is a potent EstrogenReceptor(ER)α degrader. ER degrader 6 disrupts the microtubule network by restraining tubulin polymerization. ER degrader 6 suppresses tumor growth without noticeable poisonousness .
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogenreceptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
ERα degrader 4 is an excellent and selective estrogenreceptorα (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptorα (ERRα) PROTAC degrader .
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogenreceptoralpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogenreceptor .
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptorα (ERRα) PROTAC degrader .
Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogenreceptor 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 .
Elacestrant (RAD1901) is an orally available and selective estrogenreceptor 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 .
Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogenreceptorα 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 .
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptorα (ERRα) PROTAC degrader .
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptorα (ERRα) PROTAC degrader .
AC-186 is a selective non-steroidal estrogenreceptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogenreceptorα (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
H3B-5942 is a selective, irreversible and orally active estrogenreceptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations .
Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogenreceptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
Cholesterol-d is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogenreceptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation . SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER + breast cancer .
Cholesterol-d7 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 13C3 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 13C5 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Kaempferol (Standard) is the analytical standard of Kaempferol. This product is intended for research and analytical applications. Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogenreceptorα 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 .
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
SLU-PP-332 is a pan-EstrogenReceptor/ERR agonist with EC50 values of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, respectively. SLUPP-332 enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. SLU-PP-332 has the potential to study metabolic diseases as well as improve muscle function .
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
Elacestrant-d4 (RAD1901-d4) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogenreceptor 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.
Elacestrant-d6 (RAD1901-d6) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogenreceptor 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.
(S,R,S)-AHPC-C7-amine dihydrochloride is the dihydrochloride form of (S,R,S)-AHPC-C7-amine (HY-136186). (S,R,S)-AHPC-C7-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker. (S,R,S)-AHPC-C7-amine can be used for estrogen-related receptorα (ERRα) PROTAC degrader .
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogenreceptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogenreceptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Prinaberel (ERB-041) is a potent and selective estrogenreceptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogenreceptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties .
Chlorothalonil is a broad-spectrum foliar fungicide with oral activity. Chlorothalonil can be used to combat fungal diseases in vegetable and crop leaves. Chlorothalonil can alter the microbial community in the soil. Chlorothalonil inhibits spermatogenesis. Chlorothalonil can cause intestinal epithelial barrier dysfunction and fetal toxicity .
Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Ferutinin, a natural terpenoid compound, is an estrogenreceptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca 2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities .
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogenreceptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
Isocurcumenol, an estrogenreceptoralpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively .
Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogenreceptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .
(20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogenreceptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects .
Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogenreceptorα 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 .
Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Kaempferol (Standard) is the analytical standard of Kaempferol. This product is intended for research and analytical applications. Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogenreceptorα 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 .
The ER α/ESR1 protein is a nuclear receptor that plays a critical regulatory role in gene expression, affecting cell proliferation and differentiation. Ligand-dependent transactivation involves binding of homodimers to estrogen response elements or association with transcription factors. ER alpha/ESR1 Protein, Human (His) is the recombinant human-derived ER alpha/ESR1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of ER alpha/ESR1 Protein, Human (His) is 116 a.a., with molecular weight of 12-14 kDa.
The ER α/ESR1 protein is a nuclear receptor that plays a critical regulatory role in gene expression, affecting cell proliferation and differentiation. Ligand-dependent transactivation involves binding of homodimers to estrogen response elements or association with transcription factors. ER alpha/ESR1 Protein, Human (P. pastoris, N-His) is the recombinant human-derived ER alpha/ESR1 protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of ER alpha/ESR1 Protein, Human (P. pastoris, N-His) is 586 a.a., with molecular weight of ~67.2 kDa.
Cholesterol-d7 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogenreceptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogenreceptorα (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects[1][2].
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogenreceptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogenreceptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
Cholesterol-d is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 13C3 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 13C5 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Cholesterol- 18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making 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 . Cholesterol is also an endogenous estrogen-related receptorα (ERRα) agonist .
Elacestrant-d4 (RAD1901-d4) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogenreceptor 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.
Elacestrant-d6 (RAD1901-d6) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogenreceptor 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.
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogenreceptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
Estrogen Receptor alpha Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 66 kDa, targeting to Estrogen Receptor alpha. It can be used for WB,IHC-F,IHC-P,ICC/IF,IP,ChIP assays with tag free, in the background of Human.
Estrogen Receptor alpha Antibody (YA768) is a non-conjugated and Mouse origined monoclonal antibody about 66 kDa, targeting to Estrogen Receptor alpha (6F11). It can be used for WB assays with tag free, in the background of Transfected.
