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Results for "

ER-positive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Amino Acid Derivatives (1) Androgen Receptor (1) Apoptosis (8) Autophagy (4) Bcl-2 Family (3) CDK (2) Cytochrome P450 (1) DNA/RNA Synthesis (1) Drug Derivative (1) Estrogen Receptor/ERR (15) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (5) mTOR (1) PARP (1) Potassium Channel (1) PROTACs (3) Reference Standards (1)
By Research Areas:	Cancer (27) Inflammation/Immunology (2) Metabolic Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13636

Fulvestrant Maximum Cited Publications 133 Publications Verification ICI 182780; ZD 9238; ZM 182780	Estrogen Receptor/ERR Autophagy Apoptosis	Inflammation/Immunology Cancer
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .

HY-138642

Vepdegestrant 5+ Cited Publications ARV-471	PROTACs Estrogen Receptor/ERR	Cancer
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-145572

Imlunestrant 1 Publications Verification LY-3484356	Estrogen Receptor/ERR	Cancer
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .

HY-W142080

α-Methyl-DL-tryptophan α-Methyltryptophan	mTOR Autophagy Apoptosis Amino Acid Derivatives	Metabolic Disease Cancer
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .

HY-148789

Palazestrant OP-1250	Estrogen Receptor/ERR	Inflammation/Immunology Cancer
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC₅₀ value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC₅₀ value of 1.4-1.6 nM. Palazestrant can inhibit ER ⁺/HER2 ⁺ cancer .

HY-145572A

Imlunestrant tosylate 1 Publications Verification LY-3484356 tosylate	Estrogen Receptor/ERR	Cancer
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) .

HY-13636R

Fulvestrant (Standard) Maximum Cited Publications 133 Publications Verification ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)	Reference Standards Estrogen Receptor/ERR Autophagy Apoptosis	Cancer
Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .

HY-112596

H3B-6545 3 Publications Verification	Estrogen Receptor/ERR	Cancer
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .

HY-50767S

Palbociclib-d8 PD 0332991-d₈	Isotope-Labeled Compounds CDK	Cancer
Palbociclib-d₈ is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .

HY-13636S

Fulvestrant-d3 ICI 182780-d₃; ZD 9238-d₃; ZM 182780-d₃	Isotope-Labeled Compounds Estrogen Receptor/ERR Autophagy Apoptosis	Cancer
Fulvestrant-d₃ is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .

HY-103457

Y134	Estrogen Receptor/ERR	Cancer
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 (K_i=0.09 nM) over ERβ (K_i=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .

HY-13636S1

Fulvestrant-d5 ICI 182780-d₅; ZD 9238-d₅; ZM 182780-d₅	Isotope-Labeled Compounds	Others
Fulvestrant-d₅ (ICI 182780-d₅) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.

HY-112596A

H3B-6545 hydrochloride 3 Publications Verification	Estrogen Receptor/ERR	Cancer
H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .

HY-149295

PROTAC ERα Degrader-4	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (K_i: 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.

HY-120275

CYD-2-11	Bcl-2 Family Apoptosis	Cancer
CYD-2-11 is a selective Bax agonist with a K_i value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC₅₀ values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .

HY-148368

CYD-4-61	Bcl-2 Family Apoptosis	Cancer
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .

HY-125209A

TH5427 hydrochloride	Apoptosis PARP DNA/RNA Synthesis	Cancer
TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC₅₀ of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .

HY-138642S

Vepdegestrant-d5 ARV-471-d₅	Isotope-Labeled Compounds	Cancer
Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). 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 DC₅₀ of about 2 nM .

HY-110144

TC-E 5008	Isocitrate Dehydrogenase (IDH)	Cancer
TC-E 5008 is a potent mutant IDH1 inhibitor with K_i values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a K_i value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .

HY-138642A

(Rac)-Vepdegestrant (Rac)-ARV-471	Estrogen Receptor/ERR PROTACs	Cancer
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) 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-N9174

5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone	Others	Cancer
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC₅₀ value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .

HY-50767S1

Palbociclib-d4 hydrochloride PD 0332991-d4 hydrochloride	Isotope-Labeled Compounds CDK	Cancer
Palbociclib-d₄ (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .

HY-170377

ER degrader 10	Estrogen Receptor/ERR Potassium Channel	Cancer
ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC₅₀ of 0.43 nM and an IC₅₀ of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC₅₀s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC₅₀ >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model .

HY-N8405

Isolimonexic acid	Cytochrome P450	Cancer
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC₅₀=25.60 μM) properties .

HY-168101

ERα degrader 11	Estrogen Receptor/ERR	Cancer
ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .

HY-185559

Mito-fisetin mF7	Akt Bcl-2 Family Drug Derivative	Cancer
Mito-fisetin mF7 is a lipophilic derivative of Fisetin (HY-N0182). Mito-fisetin mF7 interacts with AKT and Bcl-2, limiting their stability and functionality. Mito-fisetin mF7 stimulates impairs mitochondrial function and reduces metabolic activity of cancer cells. Mito-fisetin mF7 can be used for the research of ER-positive breast cancer .

HY-176956

ER degrader 13	Estrogen Receptor/ERR	Cancer
ER degrader 13 (Compound 37) is an estrogen receptor (ER) degrader. ER degrader 13 has a significant inhibitory effect on the proliferation of ER-positive breast cancer MCF-7 cells .

HY-182722

UT-105	Androgen Receptor	Cancer
UT-105 is an orally active androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR and promotes its degradation. UT-105 inhibits the growth of enzalutamide-resistant breast cancer xenografts and reduces tumor cell proliferation. UT-105 can be used in the research of estrogen receptor-positive breast cancer .

Cat. No.	Product Name	Target	Research Area

HY-W142080

α-Methyl-DL-tryptophan α-Methyltryptophan	mTOR Autophagy Apoptosis Amino Acid Derivatives	Metabolic Disease Cancer
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N9174

5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone	Flavonoids Flavones Plants Moraceae Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat Source Classification	Others
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC₅₀ value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .

HY-N8405

Isolimonexic acid	Natural Products Classification of Application Fields Citrus limon (L.) Burm. F. Rutaceae Plants Disease Research Fields Source Classification Cancer	Cytochrome P450
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC₅₀=25.60 μM) properties .

Cat. No.	Product Name	Chemical Structure

HY-50767S

Palbociclib-d8
Palbociclib-d₈ is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .

HY-13636S

Fulvestrant-d3
Fulvestrant-d₃ is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .

HY-13636S1

Fulvestrant-d5
Fulvestrant-d₅ (ICI 182780-d₅) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.

Fulvestrant-d5

Fulvestrant-d₅ (ICI 182780-d₅) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.

HY-138642S

Vepdegestrant-d5
Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). 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 DC₅₀ of about 2 nM .

Vepdegestrant-d5

Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). 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 DC₅₀ of about 2 nM .

HY-50767S1

Palbociclib-d4 hydrochloride
Palbociclib-d₄ (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .

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