ERα Inhibitor

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.

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 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.

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

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.

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with K_is 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 ERα^WT or ERα mutations.

AZ'6421 is an orally active ERα PROTAC degrader with a DC₅₀ of 0.4 nM. AZ'6421 recruits the VHL E3 ligase to form a ternary complex, inducing proteasome-mediated polyubiquitination and degradation of ERα. AZ'6421 inhibits the growth of ER⁺ cancer cells. AZ'6421 can be used in studies related to ER⁺ breast cancer.

Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC₅₀s of 13, 5µM for ERα and Erβ, respectively.

ERα degrader-2 is a selective estrogen receptor 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.

CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC₅₀ of 12.3 μM and a K_d of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer.

PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer.

Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC₅₀s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.

ERα-IN-3 is a ERα inhibitor with an IC₅₀ of 74.48 μM. ERα-IN-3 induces cell cycle arrest at the G0/G1 and G2/M checkpoints and triggers Apoptosis. ERα-IN-3 exhibits anticancer effects against ER-positive breast cancer. ERα-IN-3 can be used for the research of ERα-positive breast cancer.

Anticancer agent 345 is a heterobifunctional anticancer compound that exhibits weak antiproliferative activity against both ERα-overexpressing and non-overexpressing T-Rex 293 cells. Anticancer agent 345 can be used in cancer-related research.

AZD9496-O-C3-O-C3-O-C-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for ERα (HY-12870) and a PROTAC linker, which recruits E3 ligases. AZD9496-O-C3-O-C3-O-C-acid can be used for synthesis of PROTAC AZ'6421 (HY-135312).

Estrogen receptor-IN-2 is a potent estrogen receptor inhibitor formed by the conjugation of Tam (HY-13757)-NHC and gold (I). Estrogen receptor-IN-2 significantly downregulates estrogen receptor (ER) levels, inhibits ER-mediated downstream signaling pathways, and induces immunogenic cell death (ICD) mediated by damage-associated molecular patterns (DAMPs). Estrogen receptor-IN-2 can overcome drug resistance in MCF-7^Y537S mutant cells via the RAMP3/CALCR signaling pathway. It is suitable for research on endocrine-resistant breast cancer.

Anticancer agent 353 is a heterobifunctional antitumor agent with weak ERα inhibitory activity and anticancer activity. Anticancer agent 353 exhibits growth inhibitory activity against MCF7 cells. Anticancer agent 353 can be used in cancer research.

CDD-1274 is an ERα (Estrogen receptor α) variant inhibitor. CDD-1274 induces proteasomal degradation of ERα variants in breast cancer cell lines and causes Y537S ERα degradation. CDD-1274 potently blocks ligand-dependent and ligand-independent ER signaling in endocrine-resistant breast cancer cells. CDD-1274 can be used for the study of breast cancer.

ERRγ-IN-1 is a ERRγ inhibitor with an IC₅₀ of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma.

ERα-IN-2 is a ERα inhibitor. ERα-IN-2 blocks agonist-induced recruitment of nuclear receptor-binding peptides to the ligand-binding domain of ERα and exerts selective antiproliferative effects in breast cancer cells. ERα-IN-2 can be used in breast cancer-related research.

Anticancer agent 344 is a heterobifunctional anticancer compound with moderate cancer cell growth inhibitory activity, and it also exhibits inhibitory activity against ERα-overexpressing cells. Anticancer agent 344 can be used in cancer-related research.