u251

Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂，通过抑制 DNA 拓扑异构酶起抗肿瘤作用，可用于治疗卵巢癌。

Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。

JSH-23 是一种 NF-κB 抑制剂，抑制 NF-κB 转录活性 (IC50=7.1 μM)，但不影响 IκBα 降解。JSH-23 是一种抗氧化剂，具有抗炎活性。

Anisomycin 是一种由链霉菌（Streptomyces griseolus）产生的抗生素和蛋白质合成抑制剂，也是 p38 MAPK 和 JNK的经典激活剂，可通过抑制蛋白质合成引发细胞应激，激活上游激酶，进而磷酸化并激活 p38 MAPK 和 JNK。

Echinomycin (Quinomycin A) 是一种从链霉菌中分离出的抗肿瘤抗生素次级代谢物，是一种喹喔啉类抗生素，是一种 DNA 双嵌入肽，抑制低氧诱导因子-1 (HIF-1) DNA 结合活性。Echinomycin 具有潜在是抗癌活性，可用于研究三阴性乳腺癌。

Lanuginosine, an aporphine alkaloid, exhibits cytotoxicity against U251.

UniPR1454 通过靶向 EphA2 receptor 并阻断 EphA2-ephrin A1 的相互作用来发挥作用,其 IC50 值为 2.6 μM.此外,UniPR1454 能有效抑制胶质母细胞瘤细胞株 U251 的细胞增殖.

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.

Linoleic acid is an essential fatty acid and one of the most abundant polyunsaturated fatty acids in the western diet. Pyrrolidine Linoleamide is a derivative of the amide of linoleic acid that shows potent antiproliferative activity against an array of cancer cell lines, including human glioma U251 cells. It is greater than 4-fold more effective against cancer cells than non-cancer cells.

CAIX CAXII-IN-4 (Compound 7h) 是一种碳酸酐酶 (CA) 抑制剂，与CAIX、CAXII和CAII结合的Ki值分别为 1.324 μM、0.435 μM 和 3.035 μM。此化合物展示了广谱抗肿瘤作用，可抑制中枢神经系统肿瘤细胞 U251 的增殖，GI50为 0.361 μM。

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

S7是一种IL-6受体的肽类拮抗剂，能够浓度依赖性地抑制IL-6与IL-6受体的结合。在C-33 A宫颈癌细胞和RPMI-8226 B细胞淋巴细胞中，S7 (50 µM) 能抑制IL-6诱导的VEGF水平增加。在每两天给药一次，剂量为50 mg/kg的条件下，S7能减少IL-6过表达的C-33 A宫颈癌小鼠异种移植模型中的肿瘤体积。当S7与半胱氨酸结合，并连接到包裹多柔比星的脂质纳米粒子(LNPs)表面时，能增强LNPs对胶质瘤的靶向性，并在U251胶质母细胞瘤小鼠异种移植模型中提高生存率。

(S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 μM.

KY386为选择性DHX33 helicase抑制剂，IC50仅19 nM。针对U251-MG细胞（DHX33过表达癌细胞株）的抑制作用表现出相似效力，IC50为20 nM。该化合物展现出显著的抗癌活性及中等的代谢稳定性。

10m ZS44是一种能够穿透血脑屏障的Glioblastoma (GBM) 抑制剂，在小鼠异种移植模型中有效抑制了GBM肿瘤生长，并通过激活SIRT1 p53介导的细胞凋亡途径来抑制U251细胞增殖。

Ricinoleic acid is a naturally occurring 12-hydroxy fatty acid. It constitutes about 90% of the fatty acids in castor oil. Pyrrolidine Ricinoleamide is a derivative of the amide of ricinoleic acid that shows potent antiproliferative activity against an array of cancer cell lines, including human glioma U251 cells.

FAK-IN-24 (Compound 9f) 是一种FAK抑制剂，其IC50为0.815 nM。FAK-IN-24 能够诱导DNA损伤和细胞凋亡 (apoptosis)，并表现出抗胶质母细胞瘤的活性。它能够抑制U87-MG细胞系 (IC50= 15 nM) 和U251细胞系 (IC50= 20 nM) 的增殖。在U87-MG异种移植模型中，FAK-IN-24 可以有效抑制肿瘤的生长。