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OBHSA是一种选择性雌激素受体降解剂(SERD),具有针对雌激素受体α(ERα)的特异性降解活性。OBHSA对多种乳腺癌细胞的增殖具有显著抑制作用,包括对他莫昔芬敏感和抗药的乳腺癌细胞。OBHSA通过降解细胞周期蛋白D1来阻断细胞周期,从而克服他莫昔芬抗药性。OBHSA还通过诱导细胞内反应氧种的升高,触发不折叠蛋白反应(UPR)的过度激活,最终导致细胞凋亡。OBHSA显示出在发展针对内分泌抗药性乳腺癌的新型抑制药物中的巨大潜力。

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OBHSA Chemical Structure

OBHSA Chemical Structure

CAS No. : 1404508-27-5

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生物活性

OBHSA is a selective estrogen receptor degrader (SERD) with specific degradation activity against estrogen receptor α (ERα). OBHSA has a significant inhibitory effect on the proliferation of various breast cancer cells, including tamoxifen-sensitive and drug-resistant breast cancer cells. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming tamoxifen 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. OBHSA shows great potential in the development of novel inhibitory drugs against endocrine-resistant breast cancer[1].

分子量

547.54

Formula

C27H24F3NO6S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

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产品名称:
OBHSA
目录号:
HY-167701
需求量: