OBHSA
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders.
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- No. CAS: 1404508-27-5
- Fòrmula: C27H24F3NO6S
- Peso molecular:547.54
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
41.7 μM
Compound: OBHSA-1
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Cytotoxicity against human MCF10A cell incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF10A cell incubated for 72 hrs by MTT assay
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[PMID: 31437778] |
| MCF7 | IC50 |
9.84 μM
Compound: OBHSA-1
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Antiproliferative activity against human MCF7 cell incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cell incubated for 72 hrs by MTT assay
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[PMID: 31437778] |
Chemical Information
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No. CAS 1404508-27-5
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Peso molecular 547.54
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Fòrmula C27H24F3NO6S
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SMILES
FC(F)(F)CN(C1=CC=C(C=C1)OC)S(=O)([C@@H]2[C@@]3([H])C(C4=CC=C(C=C4)O)=C(C5=CC=C(C=C5)O)[C@](C2)([H])O3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. OBHSA, a novel selective estrogen receptor degrader, overcomes tamoxifen resistance through cell cycle arrest and unfolded protein response-mediated apoptosis in breast cancer [Content Brief]
[2]. Zhou J, et al. A novel selective estrogen receptor degrader induces cell cycle arrest in breast cancer via ERα degradation and the autophagy-lysosome pathway[J]. Bioorganic & Medicinal Chemistry, 2023, 82: 117235. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OBHSA Related Classifications
HY-167701 Related Classifications
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