er in mcf-7 cells

ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).ERD-308 is a highly potent PROTAC degrade

(E Z)-Droloxifene 是 (E)-Droloxifene 和 (Z)-Droloxifene 的混合物，其中 (E)-Droloxifene 是一种选择性雌激素受体调节剂。在兔子子宫匀浆实验中，(E)-Droloxifene 结合雌激素受体 (ER) 的 IC50 值为 24 nM。它能够增加未成熟大鼠的子宫重量，并减少雌二醇诱导的幼年大鼠子宫重量增加。此外，(E)-Droloxifene 抑制 17β-雌二醇刺激的 MCF-7、ZR-75-1 和 T47D 人乳腺癌细胞的生长。(Z)-Droloxifene 则由于与 ER 结合较弱，无雌激素或抗雌激素活性。

ER covalent antagonist-1 (Compound 39D) 是一种雌激素受体 α (ERα) 的拮抗剂。它可抑制 ERα 阳性细胞 MCF-7 的增殖 (IC50为 0.98 μM)，导致细胞周期在 G0 G1 期停滞，并诱导细胞发生凋亡 (apoptosis)。ER covalent antagonist-1 在小鼠模型中表现出其抗肿瘤活性。

Nur77 modulator 4 (Compound 15h) 是一种Nur77诱导剂，其KD值为0.477 μM。该化合物显著增强Nur77的表达，并诱导细胞凋亡 (Apoptosis)，在HepG2和MCF-7细胞中表现出明显的生长抑制效果，IC50均低于5 μM。Nur77 modulator 4 通过激活PERK-ATF4和IRE1信号通路来促进Nur77介导的ER应激，从而引发细胞凋亡。Nur77 modulator 4 可应用于癌症研究领域。

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

LSD1 ER-IN-1 (compound 11g) 是一种有效的 ER 和 LSD1 抑制剂，能够作用于 LSD1 (IC50: 1.55 μM)。LSD1 ER-IN-1 能够高亲和力的选择 Erα 蛋白，α β 比为 7.11。LSD1 ER-IN-1 对 MCF-7 乳腺癌细胞表现出良好的抗增殖效果 (IC50: 8.79 μM)。

D 15414 is a nonsteroidal weak estrogen of the 2-phenylindole group which was never marketed. It is the major metabolite of the selective estrogen receptor modulator zindoxifene. D-15414 has high affinity for the estrogen receptor and inhibits the growth of ER-positive MCF-7 breast cancer cells in vitro.

Pipendoxifene, also known as ERA-923, is a new antiestrogen with potential anticancer activity. ERA-923 potently inhibits estrogen binding to ER-alpha (IC50 = 14 nM). In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth (IC50 = 0.2 nM) associated with cytostasis. In vitro, a MCF-7 variant with inherent resistance to tamoxifen (10-fold) or 4-OH tamoxifen (>1000-fold) retains complete sensitivity to ERA-923 . In preclinical models, ERA-923 has an improved efficacy and safety compared with tamoxifen. In the combination with temsirolimus, ERA-923 showed excellent anticancer activity in preclinical models.

ER degrader 7 (Compound 35t) 是一种既能降解ERα又能降解ERβ的化合物。该化合物具有抑制微管蛋白聚合的功能，并能有效降低多种细胞系（包括MCF-7、T47D、MCF-10A、LCC2、T47D D538G与T47D Y537S）的细胞活性，相应IC50s值分别为0.06、2.56、15.84、1.59、1.67、1.37 μM。此外，ER degrader 7 对乳腺癌肿瘤生长同样有抑制作用。

ER degrader 9 (compound 1) 作为一种双功能分子，展现出强效的雌激素受体 (ER) 降解活性，具体表现为在 MCF-7 细胞中的 DC50 值不大于10 nM。该化合物主要应用于乳腺癌相关的科学研究。

Uralenol significantly shows the inhibitory activities against the PTP1B enzyme; it also shows inhibitory activities on mushroom tyrosinase using l-tyrosine as substrate( IC50 =49.5 μM). Uralenol shows potent anti-proliferation effects on ER-positive breast cancer MCF-7 cells in vitro.

5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone 具有抗癌活性，体外对 ER 阳性乳腺癌MCF-7细胞表现出较强的抗增殖作用，对MCF-7细胞的IC50值为4.41 uM。5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone 能显著下调雌激素受体-α (ER-α)的表达浓度，并能抑制人乳腺癌细胞系BCAP-37异种移植模型体内的肿瘤生长。

ERα17p (ERα 295-311)作为雌激素受体α (ER) 的钙调蛋白 (CaM) 结合表位，在钙依赖的方式下与CaM发生作用。该化合物通过Rho ROCK和PI3K Akt信号通路，调控包括MCF-7、SK-BR-3、T47D及MDA-MB-231在内的多种癌细胞迁移。同时，ERα17p对乳腺癌细胞的抑制作用包括减缓细胞增殖、诱发细胞凋亡 (apoptosis)，以及在小鼠模型中抑制肿瘤生长。