colon carcinoma

Aliskiren hemifumarate (CGP60536B) 一种可口服非肽肾素抑制剂，IC50为1.5 nM，具有抗高血压活性。

EIPA (L593754) 是一种 TRPP3 channel 抑制剂 (IC50=10.5 μM)，也是 Na+/H+交换 (NHE) 的抑制剂。EIPA 可以抑制巨胞饮作用，促进自噬，可用于炎症和肿瘤研究。

5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) 是一种原卟啉前体，可用作光检测器。5-ALA benzyl ester hydrochloride 在结肠癌细胞系中可以诱导原卟啉 IX (PPIX) 的积聚。

Silybin A 是水飞蓟的主要活性成分，具有抗癌和化疗预防作用，能抑制细胞增殖和迁移。

2'-Deoxyinosine (Guanine deoxyriboside) 具有 抑制人癌细胞株生长的活性，并发现其与嘌呤核苷磷酸化酶缺乏有关。

AK-1是一种特异性有效和细胞可渗透的SIRT2抑制剂，其IC50值为 12.5 μM。它可防止阿尔茨海默病模型中的海马神经退行性变并诱导结肠癌细胞中的细胞周期停滞。

Tubulin polymerization-IN-47 是一种 tubulin 聚合抑制剂和有丝分裂抑制剂，具有抗肿瘤活性，对神经母细胞瘤癌细胞增殖具有抑制作用，对 Chp-134 和 Kelly 细胞系的IC50 分别为 7 和 12 nM。Tubulin polymerization-IN-47 是治疗肝癌、结肠癌、肺癌和乳腺癌的候选化合物。

Cinnamamide is an amide of trans-cinnamic acid and a metabolite of Streptomyces. It also reduced tumor weight in a mouse model of C26 murine colon carcinoma, in vivo.

PD-1/PD-L1-IN-52 (Compound Ⅲ-5) 作为一种具有口服活性的PD-1/PD-L1抑制剂，能有效阻断PD-1与PD-L1的相互作用，其IC50值为109.9 nM。在表达人源PD-1的MC38结肠癌细胞系的C57BL/6小鼠的异种移植模型中，PD-1/PD-L1-IN-52显示出显著的抗肿瘤效果，肿瘤生长抑制率（TGI）达到49.6%。

CHI-KAT8i5 是一种高选择性的KAT8抑制剂，具有 19.72 μM 的 KD。它能以剂量依赖性方式引发凋亡 (Apoptosis)，并抑制食管鳞状细胞癌、结肠癌、黑色素瘤、胃癌、非小细胞腺癌及肝癌的肿瘤生长。

BET/Aurora kinase-IN-1 (Compound 38) 是一种双效BET/Aurora kinase抑制剂。其对多种肿瘤细胞系展现抗增殖活性，并在肾细胞癌和结肠癌的异种移植模型中表现出显著的抗肿瘤效果，肿瘤生长抑制 (TGI) 分别达到45.99%和53.06%。

KMT9-IN-1 (Compound 8) 是一种针对KMT9的抑制剂，同时也是化合物7b的乙基酯前药。此化合物在细胞中通过酯酶作用释放出活性形式7b，并与细胞内的KMT9靶向结合，降低H4K12me1水平。KMT9-IN-1 对结肠癌显示出抗肿瘤活性，并且可用于前列腺癌和肝细胞癌的研究。

Apoptosis inducer43 是一种可以引发凋亡 (apoptosis) 的试剂。它能够在 HCT116 细胞中诱导凋亡 (apoptosis)，导致 SubG0-G1 期细胞周期停滞和继发性坏死，同时上调 caspase-3、p53 及 Bax/Bcl-2 的表达。在实体艾氏癌 (SEC) 小鼠模型中，该化合物能够抑制肿瘤生长。Apoptosis inducer43 适用于结肠癌、白血病和非小细胞肺癌等癌症的研究。

Hydroquinidine hydrochloride 是有效的离子通道阻滞剂，对结肠癌、胰腺癌和肝细胞癌细胞具有显著的抗癌活性。它能延长 QT 间期，并显现出抗心律失常的效果。

TopoisomeraseI/IIα-IN-1 (Compound 20i) 是一种抑制TopoisomeraseI/IIα的化合物。MDM2-IN-27 可以有效地阻断MDM2对p53的抑制，这样激活p53信号通路。然而，MDM2-IN-27 对于乳腺癌、结肠癌和皮肤鳞状细胞癌的抗增殖活性相对较弱。

PKM2-IN-13 是一种选择性PKM2抑制剂，其对 PKM2 的IC50值为 55.13 μM。该化合物表现出广谱抗癌活性，并对正常细胞具有低毒性。PKM2-IN-13 通过增加活性氧 (ROS) 水平和激活Caspase-3/7，诱导细胞凋亡 (apoptosis)，同时在体外抑制丙酮酸激酶 M2 的糖酵解活性。其安全性较好，体内实验未发现显著不良反应。PKM2-IN-13 可用于研究口腔鳞状细胞癌、结肠癌、乳腺癌和黑色素瘤。

PFK-015 (PFK15) 是一种有效的 PFKFB3 抑制剂，对重组PFKFB3的IC50为110 nM。它能抑制 Y 细胞中的 PFKFB3 活性，IC50为20 nM。

PF04217903 是一种高效的、 ATP 竞争性的c-Met 激酶抑制剂(Ki=4.8 nM)，相对于 208 个激酶，PF04217903 显示出 1000 倍以上的选择性。它抗血管生成作用。

PHPS1 是 Shp2的选择性抑制剂，对 Shp2，Shp2-R362K，Shp1，PTP1B 和 PTP1B-Q 的 Ki 分别为 0.73，5.8，10.7，5.8 和 0.47 μM。

Monoacylglycerols (MAGs) of ω-3 polyunsaturated fatty acids have diverse physiological and health effects. In particular, MAGs containing docosahexaenoic acid or eicosapentaenoic acid have anti-proliferative properties against colon and lung cancer cell lines. Eicosapentaenoyl 1-propanol-2-amide is an EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 μM. It is an analog of eicosapentaenoyl ethanolamide , a natural N-acylethanolamide that impacts aging and inflammation.

1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0/G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

Neoanhydropodophyllol, a cyclolignan derivative, exhibits potent antineoplastic activity by exerting cytotoxic effects on various cancer cell lines including leukemia, lung carcinoma, and colon carcinoma.