T73458
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LWG-301是一种针对Glutaminase1(GLS1)的变构抑制剂,具有(IC50=7 nM)。通过显著阻断谷氨酰胺代谢并增加细胞内ROS,LWG-301能够诱导细胞凋亡(apoptosis)。在HCT116异种移植模型中,LWG-301展示出中等抗肿瘤活性。 |
T74454
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JPS016 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS016 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS016 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 |
T77937
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HDAC
PROTACs
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JPS014 TFA是一种VHL E3连接酶蛋白水解靶向嵌合体(PROTAC),以苯甲酰胺为基础,专门降解I类组蛋白脱乙酰酶(HDAC)。作为一种高效的HDAC1/2降解剂,JPS014 TFA与HCT116细胞中广泛的基因表达差异及促进细胞凋亡(apoptosis)密切相关。 |
T79327
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EGFR
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EGFR-IN-81(Compound 10i)是一种选择性EGFR抑制剂,针对EGFRWT和L858R/T790M的抑制作用表现IC50值分别为4.38 nM和5.69 nM。此外,EGFR-IN-81对MCF-7和HCT116细胞株展示了细胞毒性,其有效浓度分别达到2.07 μM和6.72 μM。 |
T39200
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β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of colorectal cancer cells SW480 and HCT116, with IC50 values of 20 μM and 31 μM, respectively. |
T61996
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Antiproliferative agent-6 (compound 8a) 是有效的抗肿瘤化合物。Antiproliferative agent-6 具有抗增殖活性,抑制癌细胞系 HCT116、MCF-7、H460 和非肿瘤非整倍体永生角质细胞 HaCaT 的 GI50分别为 0.5 μM、2 μM、0.7 μM 和 3.5 μM。 |
T83011
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Antitumor agent-105(Compound 37)是一种对A549、H1299、H460、HCT116、MDA-MB-231细胞线显示出抗肿瘤活性的化合物,其IC50值分别为6.7、8.3、4.3、4.4、6.7μM。 |
T37584
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Tryptoquivaline D is a fungal metabolite that has been found inNeosartorya siamensisand has anticancer activity.1,2It induces nuclear chromatin condensation, a marker of apoptosis, in HCT116 colon and HepG2 liver cancer cells when used at a concentration of 150 μM.1Tryptoquivaline D (1-100 μM), alone or in combination with doxorubicin , reduces the viability of A549 lung cancer cells.2 |
T36627
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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. |
T38381
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CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg.
1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020) |