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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- CAS No.: 1404508-27-5
- Formule: C27H24F3NO6S
- Masse moléculaire:547.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
41.7 μM
Compound: OBHSA-1
|
Cytotoxicity against human MCF10A cell incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF10A cell incubated for 72 hrs by MTT assay
|
[PMID: 31437778] |
| MCF7 | IC50 |
9.84 μM
Compound: OBHSA-1
|
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
|
[PMID: 31437778] |
Chemical Information
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CAS No. 1404508-27-5
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Masse moléculaire 547.54
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Formule 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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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
[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)