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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

ER-positive breast cancer cells

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Amino Acid Derivatives (1) Androgen Receptor (1) Apoptosis (3) Autophagy (1) Bcl-2 Family (2) DNA/RNA Synthesis (1) Drug Derivative (1) Estrogen Receptor/ERR (8) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (1) mTOR (1) PARP (1) PROTACs (2)
By Research Areas:	Cancer (16) Inflammation/Immunology (1) Metabolic Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: BCRP Nuclear Factor of activated T Cells (NFAT) BRK TREM receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-138642

Vepdegestrant Maximum Cited Publications 6 Publications Verification 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-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-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-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-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-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 .

Cat. No.	Product Name	Chemical Structure

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 .

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