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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1404508-27-5
- 分子式: C27H24F3NO6S
- 分子量:547.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
|
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] |
化学情報
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CAS 番号 1404508-27-5
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分子量 547.54
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)