4t1 breast cancer cells

WRG-28 是一种选择性的、细胞外作用的DDR2变构抑制剂 (IC50:230 nM)。它通过受体的变构调节特异地抑制受体-配体相互作用。它通过靶向 DDR2 抑制肿瘤侵袭和迁移，基质的肿瘤支持作用，能够抑制肺中的转移性乳腺肿瘤细胞定植。

CAR-2 是一种源于 BODIPY 的光敏剂，能通过靶向内质网 (ER) 和脂滴 (LD) 在光动力疗法 (PDT) 中诱导铁死亡 (ferroptosis)。其在乳腺癌细胞中显示出光毒性，IC50为 0.01-0.02 μM。此外，CAR-2 在 4T1 异种移植小鼠模型中展现了抗肿瘤功效。

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3 Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB c mice with a dose of 1 mg kg of 3,5-dimethyl PIT-1 per day.

Nifuroxazide-d4 is intended for use as an internal standard for the quantification of nifuroxazide by GC- or LC-MS. Nifuroxazide is a nitrofuran antibiotic. It is active against strains of the enteropathogenic bacteria C. jejuni, Salmonella, Y. enterocolitica, Shigella, and E. coli. It inhibits quorum sensing and virulence factor production in P. aeruginosa. Nifuroxazide inhibits STAT3 activity in a reporter assay and decreases viability of U266 and INA-6 myeloma cells, which have constitutive STAT3 phosphorylation, with EC50 values of approximately 4.5 µM for both. It also decreases viability, migration, and invasion of, and induces apoptosis in, MCF-7, 4T1, and MDA-MB-231 breast cancer cells. Nifuroxazide reduces tumor growth and prevents pulmonary metastasis in a 4T1 murine mammary carcinoma model. It also reduces diarrhea, weight loss, and colon inflammation in a rat model of acetic acid-induced ulcerative colitis.

Antitumor agent-115 (SS-12)是一种在体外展现出显著抗肿瘤活性的化合物，针对小鼠乳腺癌细胞系4T1的IC50值介于0.34 μM至24.14 μM。该化合物能够阻断4T1细胞周期、降低其线粒体膜电位并诱导凋亡，其对4T1细胞抑制活性的IC50值在8-25 μmol L之间，适用于乳腺癌研究领域。

HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂，IC50值为14 nM，针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示，对4T1细胞株的IC50为0.55 μM，对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平（如H3K9、H3K27和H4K12），促进细胞凋亡（涉及caspase-3、caspase-7和细胞色素c的水平提升），并抑制细胞增殖相关蛋白（如Bcl-2、CD44、EGFR和Ki-67）的表达，从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。

Anticanceragent 33 (compound 3) 为Squamocin与Bullatacin衍生物，展现出有效的抗癌特性。本化合物对4T1乳腺癌细胞系（包括A549、HeLa、HepG2和MCF-7细胞）的生长抑制作用显著，其IC50范围为1.9-5.4 µM。

LLK203是一种有效的USP2 USP8双靶点抑制剂，IC50分别为0.89 μM和0.52 μM。LLK203导致ERα降解并诱导乳腺癌MCF-7细胞凋亡，对4T1肿瘤小鼠模型具有抗肿瘤活性。