hct-15

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。

ZINC05007751 是 NIMA 相关激酶 NEK6 的有效抑制剂（IC50 = 3.4 μM）。 ZINC05007751 对 NEK1 和 NEK6 具有很强的特异性，对 NEK2、NEK7 和 NEK9 没有显着的活性。

Defactinib (VS-6063) 是一种 FAK 的第二代抑制剂，抑制 FAK 在 Tyr397 位点磷酸化。Defactinib 具有潜在抗肿瘤活性。

Cyclophosphamide 是一种烷化剂，具有抗肿瘤及免疫抑制活性，用于治疗多种癌症。

Gallic acid (Benzoic acid) 属于天然多羟基酚类，可以抑制 COX-2 的自由基清除作用。Gallic acid 具有抗氧化、抗炎、抗肿瘤、抗菌等多种生理活性。

Irinotecan (CPT-11) 是喜树碱的衍生物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接，并导致双链 DNA 断裂和细胞死亡，具有抗肿瘤活性。

Selisistat (EX-527) 是一种去乙酰化酶 SIRT1 的抑制剂 (IC50=38 nM)，具有有效性和特异性。Selisistat 可以用于神经系统疾病如亨廷顿舞蹈病的研究。

Mertansine 是一种微管蛋白抑制剂，也是一种抗体可缀合的美登木素生物碱。Mertansine 对HCT-15和A431细胞的IC50分别是0.750和0.04nM。

Mertansine (GMP)是 Mertansine 的 GMP 级别试剂。Mertansine 是一种微管蛋白抑制剂，也是一种抗体可缀合的美登木素生物碱。Mertansine 对HCT-15和A431细胞的IC50分别是0.750和0.04nM。

TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.

RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA DX5, HCT-15, and HCT-15 CLO2 cells [1].

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.

Kinetin riboside (N6-Furfuryladenosine) 是一种细胞分裂素类似物，可诱导癌细胞凋亡， 抑制 HCT-15 细胞的增殖，IC50 为 2.5 μM。

Angiogenesis inhibitor 3 (compound 8) 是一种有效的血管生成(angiogenesis)抑制剂，能够抑制HUVEC和HCT-15细胞增殖，其IC50值分别为1.00和0.71 μM。此外，此化合物还能诱导这两种细胞的凋亡(apoptosis)并具有抑制癌细胞侵袭的抗癌活性。Angiogenesis inhibitor 3还能够抑制斑马鱼胚胎的血管生成。

WES-1（Compound 8g）是一种针对碳酸酐酶IX的抑制剂，其抑制常数（Ki）为55.9 μM。该化合物对包括白血病细胞系（K-562、MOLT-4）、非小细胞肺癌（NCI-H460）、结肠癌（HCT 116、HCT-15）以及黑色素瘤（LOX IMVI）在内的多种癌细胞表现出抗增殖效果。

SLU-10482是一种抗寄生虫化合物，能减少HCT-8细胞中C. parvum寄生虫的数量（EC50 = 0.07 µM）。相较于另一种抗寄生虫化合物SLU-2633，SLU-10482与人类ether-a-go-go (hERG; Kd = 43 µM)的结合能力较弱。在体内，SLU-10482以5和15 mg/kg的剂量，每天两次给药，能减少C. parvum感染小鼠模型中粪便中卵囊的数量。

化合物C3N-Dbn-Trp2 作为ATP结合盒转运蛋白ABCB1的抑制剂, 在HEK293T及HCT-15细胞中，该化合物阻断了ABCB1介导的Rhodamine 123的外排作用，其IC50值分别为5.9 µM和2.2 µM。此外，C3N-Dbn-Trp2 还能抑制Doxorubicin的外排，从而提高了ABCB1表达细胞对Doxorubicin的细胞毒性响应。

hDHODH-IN-15 (Compound H19) 作为人二氢鸟苷酸脱氢酶(hDHODH)的抑制剂,具有 0.21 µM 的 IC50 值.在癌细胞系包括 NCI-H226、HCT-116 和 MDA-MB-231 中,通过促进铁死亡(ferroptosis),展现出 0.95-2.81 µM 范围的 IC50 值,具备良好的细胞毒性和抗肿瘤效果.

Antitumor agent-182 (Compound 12a) 在降低线粒体膜电位 (MMP) 的同时,能有效提升ROS水平.该化合物通过在G0 G1期阻断细胞周期来诱导HeLa细胞的凋亡(apoptosis).此外,Antitumor agent-182 对HeLa、PC-3 和 HCT-15细胞系表现出显著的抑制作用,其IC50值分别为8.83、10.07 和 7.84 μM.

Cnidicin 是一种香豆素，对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。

3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, and 3beta-O-trans-p-coumaroyltormentic acid are weakly selective for vancomycin-resistant Enterococcus (VRE) compared with eukaryotic cells, with an MIC of 59.4microg mL and a 50% inhibitory concentration (IC50) of 72.0microg mL for monkey kidney epithelial (MA104) cells. A mixture of 3-O-cis-p-coumaroyltormentic acid and 3-O-trans-p-coumaroyltormentic acid shows an inhibitory effect comparable to (-)-epigallocatechin gallate (EGCG) of green tea on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradeca--noylphorbol-13-acetate (TPA).

7-Hydroxycadalene shows cytotoxicity activity against HCT-15 cell line with IC50 18.89 ± 1.2 uM.

Coccinic acid shows inhibitory effects against colorectal carcinoma HCT-15 and oral epithelial cell line KB-3-1.Mixture of coccinic acid and anwuweizonic acid shows significant inhibitory activity against human decidual cells and rat luteal cells in vitro

Schizandriside may have anti-inflammatory effects, it has inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells. It shows significant cytotoxicity against A549, SK-OV-3, SK