breast epithelial

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

SMIFH2 is formin homology 2 (FH2) domains inhibitor.

LG100268 is a potent, selective, and orally active retinoid X receptor (RXR) agonist that agonizes RXR-α, RXR-β, and RXR-γ at the nanomolar level, selectively exceeding the RAR by three orders of magnitude.LG100268 is capable of inducing transcriptional activation in adipocytes; affecting the RXRs and their chaperone receptor, Foxl2 Dmrt1, to induce flounder masculinization in juvenile flounder; inhibits keratin 17 expression in nigrostriatal epithelial cells; and increases PD-L1 expression in HER2 or triple-negative breast cancer.

LA-CB1 is a derivative of Abemaciclib that targets CDK4/6 and promotes their degradation via the ubiquitin-proteasome pathway, thereby blocking the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis (Apoptosis). It demonstrates antiproliferative activity against MDA-MB-231 cells with an IC50 of 0.27 µM and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In highly invasive models like triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth, showing robust dose-dependent antitumor activity. This compound can be utilized in breast cancer research.

trans-Trimethoxyresveratrol (MR-3), a natural methoxylated analog of resveratrol, inhibits breast Y cell invasiveness by downregulation of PI3K/Akt and Wnt/β-catenin signaling cascades and reversal of epithelial-mesenchymal transition.

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 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs.

Goserelin acetate (Fertilan) is a synthetic long-acting agonist of gonadotropin-releasing hormone, used in treatments of cancer.

Enterolactone (trans-α,β-Bis(3-hydroxybenzyl)butyrolactone) is a bioactive phenolic metabolite with estrogenic properties and anti-breast cancer activity. It strongly inhibits cancer cell proliferation and migration by upregulating THBS1, synergistically suppressing epithelial ovarian cancer.

1. Obtusifolin has antioxidant properties and improves chemically induced diabetes and its complications by modulation of oxidative stress. 2. Obtusifolin suppresses phthalate esters-mediated bone resorption, thus may be a novel anti-breast-cancer bone me

HSP90-IN-10 is a potent inhibitor of HSP90. HSP90-IN-10 exhibits potent anti-proliferative effects on HCC1954 breast cancer cells (IC50: 6 μM). hSP90-IN-10 induces apoptosis without inhibiting the growth of normal epithelial cells.

JMX0293, an O-alkylamino-tethered salicylamide derivative, demonstrates strong efficacy against the TNBC MDA-MB-231 cell line with an IC50 of 3.38 μM, while showing minimal toxicity towards the non-tumorigenic human breast epithelial cell line MCF-10A, where its IC50 exceeds 60 μM. It inhibits STAT3 phosphorylation, contributing to apoptosis in MDA-MB-231 cells, and significantly suppresses MDA-MB-231 xenograft tumor growth in vivo, all without notable toxicity.

Tarextumab (OMP-59R5) is a fully human IgG2 monoclonal antibody designed to selectively target and inhibit the signaling of Notch2 and Notch3 receptors. preclinical and clinical studies have demonstrated that inhibition of the Notch2/3 pathway with chemotherapeutic agents is efficacious across a broad spectrum of epithelial tumors, including breast, lung, ovarian, and pancreatic cancers, thereby establishing Tarextumab as a promising candidate for oncological research and development.

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits epithelial-mesenchymal transition through the Wnt β-catenin signaling pathway, thereby inhibiting migration and invasion of human breast cancer cells.

3,6-Dihydroxyflavone suppresses the epithelial-mesenchymal transition in breast cancer cells by inhibiting the Notch signaling pathway.

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.

P-XSC has anticancer activity, inhibits proliferation of colonic epithelial cells in patients with adenomatous polyps, and may be used in the study of breast cancer.

AW01178, an HDAC inhibitor, induces upregulation of E-cadherin mRNA and protein levels, thereby inhibiting epithelial-mesenchymal transition in breast cancer cells.