hct-116 cells

5-fluorouridine is also known as FUrd, 5-Fluorouracil 1-beta-D-ribofuranoside, 5-Fur, or 5-Fluoro-uridine. 5-fluorouridine is a solid. This compound belongs to the pyrimidine nucleosides and analogues. These are compounds comprising a pyrimidine base attached to a sugar. 5-fluorouridine is known to target uridine phosphorylase. FUrd is often used in chemical and biochemical comparison studies with fluorouracil and thymine analogs.

ARM1 is a potent inhibitor of aminopeptidase and epoxide hydrolase. The IC50 values are 7.61 µM for aminopeptidase and 12.4 µM for epoxide hydrolase.

Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.

Arcyriaflavin A is derived from Eudistoma sp. It inhibits D1-CDK4, B-CDK1 and CaMKII with IC50 values ​​of 0.14μM, 1.13μM and 0.025μM, respectively. Arcyriaflavin A also inhibits HCT-116 and NCI-H460 cells with IC50 values ​​of 0.85μM and 0.59μM, respectively.

3'-Hydroxypterostilbene (3'-HPT), a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells with IC50s of 9.0, 40.2, and 70.9 μM for COLO 205, HCT-116, and HT-29 cells, respectively, by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the p38MAPK , and PI3K/Akt/mTOR/p70S6K pathways and activates the ERK1/2, JNK1/2 MAPK pathways[1].

RLX HCl is a narcissus ketone analogue with anticancer activity that inhibits tumour proliferation by suppressing the PI3K Akt FoxO3a signalling pathway in experimental colon cancer, downregulating the p110α and p85 subunits of PI3K in HCT-116 cells, and exhibiting antiproliferative effects.

3-arylisoquinolinamine derivative is a compound with antitumor activity.

MSN-125 effectively inhibits Bax Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond

PROTACKSP-IN-1 (Compound 21) is a spindle protein (KSP) degrader as a PROTAC, effectively degrading KSP in HCT-116 cells with a DC50 value of 114.8 nM. It inhibits the proliferation of HCT-116 with an IC50 of 10 nM, causes G2 M phase cell cycle arrest, and induces apoptosis in HCT-116. Additionally, PROTACKSP-IN-1 demonstrates antitumor activity in mouse models.

LSD1 HDAC-IN-2 (Compound 20c) acts as an inhibitor targeting both LSD1 and several HDACs, specifically HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50 values of 39.0, 1.4, 1.0, 1.3, 2.9, and 16.0 nM, respectively. This compound effectively inhibits the proliferation of cancer cells, notably colorectal cancer cells. LSD1 HDAC-IN-2 induces cell cycle arrest at the G2 M phase, inhibits cell migration, and triggers apoptosis in HCT-116 and HT-29 cells. Additionally, it demonstrates antitumor activity in mouse models without causing significant toxicity at a dose of 20 mg kg.

MAPK-IN-3 (Compound 4a) is an antiproliferative agent demonstrating significant inhibitory effects on KYSE 30, HCT 116, and HGC 27 cell lines, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. This compound arrests the cell cycle via a p53-dependent mechanism and induces apoptosis through a p53-independent pathway. It reduces the expression of cell cycle-related proteins, such as Cyclin D1 and Cyclin B1, while increasing pro-apoptotic proteins like cleaved PARP, cleaved caspase-7, and cleaved caspase-9. MAPK-IN-3 also decreases anti-apoptotic proteins such as Bcl-2, elevates ROS levels in KYSE 30 cells, and enhances the expression of ROS-related MAPK pathway members, including p-ERK, p-p38, and p-JNK.

Anticanceragent 260 (Compound 3g 4d) is an orally effective anticancer agent that inhibits the proliferation of cancer cells HCT-116, MIA-PaCa2, and MDA-MB231, with IC50 values of 98.7, 81.0, and 77.2 µg mL, respectively. It also promotes ulcer formation and lipid peroxidation, and exhibits anti-inflammatory and analgesic activities.

NPC26 is a small molecule that disrupts mitochondrial function and exhibits antitumor activity. It shows significant antiproliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 induces mitochondrial permeability transition pore (mPTP) opening, generates reactive oxygen species (ROS), and triggers cell death. Additionally, NPC26 kills CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway.

MAT2A-IN-16 is a MAT2A inhibitor that effectively suppresses the proliferation of MTAP- -HCT-116 cells, with an IC50 value of 20 nM.

HDAC1-IN-9 (13c) is an HDAC1 inhibitor. It inhibits the HDAC1 enzyme with an IC50 value of 1.07 µM. This compound exhibits the strongest antiproliferative activity against HT-29 (human colon adenocarcinoma cells), with an IC50 of 1.78 μM. In HCT-116 (human colon cancer cells), HDAC1-IN-9 significantly induces apoptosis. Additionally, HDAC1-IN-9 possesses antiangiogenic properties, reducing the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80%.

Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.

HDAC6-IN-56 (compound 18d) is an inhibitor of HDAC6, with an IC50 of 1.3 nM. This compound can inhibit the S phase and induce apoptosis in HCT-116 colon cancer cells.

DDO-6691 is an inhibitor of heat shock protein 90 (HSP90). It exhibits antiproliferative effects against various tumor cells, with the highest sensitivity observed in HCT-116 colon cancer cells (IC50: 1.08 μM). DDO-6691 also demonstrates potent tumor growth inhibition in HCT-116 xenograft mouse models.

Erysolin is a natural product with anti-cancer potential. It is cytotoxic to a variety of cancer cells (DU145, HCT 116, MCF7, HEP3B, SKOV3, SF-268) and has antibacterial activity against Escherichia coli.

3-O-acetyloleanolic acid dose-dependently inhibited the viability of HCT-116 cells. Apoptosis was characterized by detection of cell surface annexin V and sub-G1 apoptotic cell populations.

1. β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) is a promising agent for developing an improved strategy for radiotherapy against tumors. (a) Injection of Dimethylacrylshikonin combined with IR treatment significantly suppressed tumor growth of the HCT-116 xenograft. (b) Dimethylacrylshikonin significantly suppressed the growth of H(22) transplantable hepatoma, and induced the activation of caspase-3 . (c) Dimethylacrylshikonin inhibited growth of gastric cancer SGC-791 cells by inducing ERK signaling pathway. 2. Dimethylacrylshikonin inhibits the proliferation of MCF-7 cells in vitro by inducing apoptosis through the downregulation of Bcl-2, upregulation of Bax and partial inactivation of the NF-κB pathway.

B-Raf IN 8 (compound 7g) is a potent inhibitor of B-Raf (IC50 = 70.65 nM) with antitumor activity, demonstrating IC50 values of 9.78, 13.78, 18.52, and 29.85 μM against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7), and human prostate cancer (PC-3) cells [1].

B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor with an IC50 of 110.23 nM. It exhibits antitumor activity against colon carcinoma cells (HCT-116), mammary gland cells (MCF-7), hepatocellular carcinoma cells (HEPG-2), human cervical carcinoma cells (Hela), and human prostate cancer cells (PC-3), with IC50 values of 7.50, 9.87, 10.57, 11.63, and 12.83 μM, respectively [1].

PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor with an IC50 of 0.67 μM, and it also shows notable cytotoxicity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively [1].