Estrogen receptor-IN-2
Estrogen receptor-IN-2 is a potent estrogen receptor inhibitor formed by the conjugation of Tam-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-7Y537S mutant cells via the RAMP3/CALCR signaling pathway. It is suitable for research on endocrine-resistant breast cancer.
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- Formule: C55H63AuBr2N5O5
- Masse moléculaire:1230.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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JNK |
p38 |
ERαY537S |
ERαWT |
ERRα |
Estrogen receptor |
GRP78 |
Estrogen receptor-IN-2 (compound 7b) (72 h) exhibits significant antiproliferative activity in MCF-7 cells (IC50 = 0.38 μM) and Ishikawa cells (IC50 = 0.75 μM)[1].
Estrogen receptor-IN-2 (120 h) demonstrates antiproliferative activity that overcomes endocrine resistance in MCF-7Y537S cells (IC50 = 0.16 μM) and MCF-7D538G cells (IC50 = 0.52 μM)[1].
Estrogen receptor-IN-2 (0.5-4 μM; 24 h) downregulates ERα protein expression in MCF-7 cells[1].
Estrogen receptor-IN-2 (24 h) antagonizes ERE transcriptional activity in MCF-7 cells[1].
Estrogen receptor-IN-2 (0.5-2 μM; 24 h) inhibits the expression of ER downstream genes (PR and TFF-1) in MCF-7 cells. Estrogen receptor-IN-2 inhibits thioredoxin reductase (TrxR) activity in a dose-dependent manner in MCF-7 cells. Estrogen receptor-IN-2 activates the ASK1/JNK/p38 signaling pathway in MCF-7 cells[1].
Estrogen receptor-IN-2 (12 h) induces specific mitochondrial and cytoplasmic distribution in MCF-7 cells[1].
Estrogen receptor-IN-2 (0.5-4 μM; 12 h) increases intracellular reactive oxygen species (ROS) levels in MCF-7 cells. Estrogen receptor-IN-2 induces a decrease in mitochondrial membrane potential and mitochondrial dysfunction in MCF-7 cells. Estrogen receptor-IN-2 triggers the release of intracellular calcium ions in MCF-7 cells[1].
Estrogen receptor-IN-2 (0.5-4 μM; 24 h) induces endoplasmic reticulum stress (ERS) in MCF-7 cells. Estrogen receptor-IN-2 causes cell cycle arrest at the G0/G1 phase and induces apoptosis in MCF-7 cells[1].
Estrogen receptor-IN-2 (4 μM; 3-24 h) induces the release of immunogenic cell death (ICD) markers in MCF-7 cells[1].
Estrogen receptor-IN-2 (2-10 μM; 24 h) downregulates the drug resistance-associated RAMP3/CALCR signaling pathway and gene expression in MCF-7Y537S cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 h
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Result:Downregulated the ERα protein level in a dose-dependent manner.
Increased the ratios of p-ASK1/ASK1, p-JNK/JNK, and p-p38/p38, activating the downstream pathway.
Upregulated the expression of endoplasmic reticulum stress-related proteins (Calnexin, GRP78, ATF-4, and CHOP), as well as CRT and HMGB1.
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Cell Line:MCF-7 cells, MCF-7Y537S cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Inhibited the expression of PR and TFF-1 genes.
Significantly reduced the expression of resistance-associated RAMP3 and CALCR genes.
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Cell Line:MCF-7 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:12 h, 24 h
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Result:Decreased ER protein levels.
Increased ROS levels.
Increased the expression of endoplasmic reticulum stress markers such as Calnexin and GRP78.
Promoted HMGB1 release and CRT cell membrane exposure.
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Cell Line:MCF-7 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 h
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Result:Resulted in cell cycle arrest at the G0/G1 phase.
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Cell Line:MCF-7 cells
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner.
Estrogen receptor-IN-2 (10 mg/kg; i.p.; every other day; for 24 days) exhibits the activity to overcome drug resistance, significantly inhibit tumor growth, and downregulate the expression of ER, PR, and Ki67 in tumor tissues in female BALB/c nude mice (42-48 days old, subcutaneous mutant MCF-7Y537S xenograft model)[1].
Estrogen receptor-IN-2 (10 mg/kg; i.p.; once a day; for 2 days) demonstrates a good safety profile in immature female SD rats (weighing approximately 100 g)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (42-48-day-old, female) were inoculated subcutaneously with 1 × 106 wild-type MCF-7 cells[1].
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Dosage:10 mg/kg
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Administration:i.p.; every other day; for 24 days
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Result:Significantly inhibited tumor growth and decreased tumor volume and weight.
Caused no obvious mouse body weight loss or morphological damage to organs (heart, liver, spleen, lung, kidney)
Significantly downregulated the expression levels of ER, PR, and Ki67 in tumor tissues.
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Animal Model:BALB/c nude mice (42-48-day-old, female) were inoculated subcutaneously with 1 × 106 mutant MCF-7Y537S cells[1].
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Dosage:10 mg/kg
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Administration:i.p.; every other day; for 24 days
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Result:Overcame endocrine resistance and significantly inhibited mutant tumor growth and significantly decreased tumor volume and weight.
Caused no obvious mouse body weight loss or organ damage during treatment.
Significantly downregulated the expression levels of ER, PR, and Ki67 in tumor tissues.
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Animal Model:SD rats (immature female, approximately 100 g) [1].
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Dosage:10 mg/kg
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Administration:i.p.; once daily; for 2 days
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Result:Reduced the uterine wet weight.
Exhibited no significant estrogenic agonistic effects, indicating a good safety profile.
Chemical Information
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Masse moléculaire 1230.89
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Formule C55H63AuBr2N5O5
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SMILES
CN(CCOC1=CC=C(/C(C2=CC=CC=C2)=C(CC)\C3=CC=CC=C3)C=C1)C(OCCC[N+]4=C([Au]C5=[N+](CC)C(C6=CC=C(OC)C=C6)=C(C7=CC=C(OC)C=C7)N5CC)N(CC)C=C4)=O.[Br-].[Br-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Estrogen receptor-IN-2 Related Classifications
HY-184982 Related Classifications
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