breast epithelial

KPT-6566 是共价结合的脯氨酰异构酶PIN1选择性抑制剂，能够与 PIN1 的催化位点共价结合，抑制并降解PIN1，具有抗癌活性。它对PIN1 PPIase 结构域的IC50=640 nM，Ki=625.2 nM。

Berberine (Umbellatine) 属于生物碱类天然产物，可以激活 AMPK、抑制 DNA 拓扑异构酶、诱导 ROS 生成。Berberine 具有抗肿瘤、抗菌、降血糖、降血脂等生物学活性。

SMIFH2 是formin 特异性抑制剂。它利用 Formins 阻碍肌动蛋白聚合，影响肌动蛋白细胞骨架。

LG100268是一种强效、选择性和口服活性的视黄醇X受体（RXR）激动剂，以纳摩尔级别激动RXR-α、RXR-β和RXR-γ，选择性超过RAR三个数量级。LG100268能够诱导脂肪细胞中的转录激活；影响RXRs和其伴侣受体Foxl2 Dmrt1诱导比目鱼幼鱼的雄性化；抑制黑脂腺上皮细胞中角蛋白17的表达；在HER2或三阴性乳腺癌中增加PD-L1的表达。

trans-Trimethoxyresveratrol (MR-3) 是一种 Resveratrol(RSV) 的衍生物，与Resveratrol(RSV)相比，它可能是一个更有效的抗炎、抗血管新生的化合物。

CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16 F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16 F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg kg) reduces tumor growth in B16 F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16 F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16 F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg kg) reduces tumor growth in B16 F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

C22 Sphingomyelin is a naturally occurring form of sphingomyelin . Plasma levels of C22 sphingomyelin positively correlate with hepatic steatosis severity in patients with chronic hepatitis C virus (HCV). C22 Sphingomyelin levels are decreased in T-47D mammary epithelial cells and increased in MDA-MB-231 breast cancer cells relative to C16 sphingomyelin .

C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7 Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation, enhances cAMP-activated chloride secretion, and suppresses secretion of IL-8 in primary epithelial cells isolated from patients with cystic fibrosis.[3]

EW-7195 是一种具有选择性和高效性的 ALK5 (TGFβR1) 抑制剂，IC50 值为 4.83 nM。EW-7195 对 ALK5 的亲和力是 p38α 的 300 多倍。EW-7195 对 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移有抑制作用。

Goserelin acetate (Fertilan) 是一种促性腺激素释放激素 (GnRH LHRH) 十肽类似物，能作为GnRH 激动剂。它可研究乳腺癌、上皮性卵巢癌和前列腺癌。

Enterolactone (trans-α,β-Bis(3-hydroxybenzyl)butyrolactone) 是一种生物活性酚类代谢物，具有雌激素特性和抗乳腺癌活性，对癌细胞增殖和迁移具有很强的抑制活性，通过上调 THBS1 协同抑制上皮性卵巢癌。

Obtusifolin 是分离自决明子的种子中，能够抑制NF-kB 通路，调节气道上皮细胞中 MUC5AC 粘蛋白的基因表达和产生。它通过靶向甲状旁腺激素相关蛋白来抑制邻苯二甲酸酯诱导的乳腺癌骨转移。

HSP90-IN-10 是 HSP90 的有效抑制剂。HSP90-IN-10 对 HCC1954 乳腺癌细胞表现出强大的抗增殖效果 (IC50: 6 μM)。HSP90-IN-10 能够诱导细胞凋亡 (apoptosis)，且不抑制正常上皮细胞的生长。

JMX0293是一种O-烷基氨基连接的水杨酰胺衍生物化合物，具有针对MDA-MB-231细胞系的高效力(IC50=3.38 μM)，且对MCF-10A人非致瘤性乳腺上皮细胞系的毒性极低(IC50>60 μM)。该化合物能抑制STAT3磷酸化，促进TNBC MDA-MB-231细胞的凋亡，同时在体内显著抑制MDA-MB-231异种移植肿瘤的生长，无明显毒性。

FL118是一种新型存活素抑制剂，可抑制癌症干细胞样特性。FL118 是一种新型喜树碱类似物，具有抗癌活性，通过 Wnt β-catenin 信号通路抑制上皮-间充质转化，从而抑制人乳腺癌细胞的迁移和侵袭。

3,6-Dihydroxyflavone 是一种抗癌剂。它能够提高细胞内氧化应激和脂质过氧化。它是能够根据剂量和时间依赖性地降低细胞活力，并活化半胱天冬酶级联、切割聚 (ADP-核糖) 聚合酶 (PARP) 诱导细胞凋亡。

Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2.5 µM时诱导这些细胞类型的自噬细胞死亡。DDA (0.37 µg/kg)在B16/F10小鼠黑色素瘤模型和TS/A小鼠乳腺癌模型中减缓肿瘤生长，并在体内外诱导癌细胞分化。

P-XSC 具有抗癌活性，抑制腺瘤性息肉患者结肠上皮细胞增殖，可用于研究乳腺癌。

AW01178 是一种HDAC抑制剂，能够诱导 E-cadherin mRNA 和蛋白水平的上调，并抑制乳腺癌细胞的上皮-间充质转化。