sw480

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

Teplinovivint is a potent inhibitor of the Wnt/β-catenin signaling pathway, demonstrating anti-inflammatory properties with potential utility in tendinopathy research.

Adavivint (SM04690) is a selective inhibitor of the typical Wnt signaling pathway. In SW480 cells, EC50=19.5 nM was measured using high-throughput TCF/LEF reporter gene experiments.

MS-444 (BE-34776) is a smooth muscle myosin light chain kinase (MLCK) and HuR inhibitor with antitumor activity for triple-negative breast and colorectal cancer.

5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) is a protoporphyrin precursor used as a photodetection agent. It induces protoporphyrin IX (PPIX) accumulation in colon carcinoma cell lines.

SFI003 is a novel SRSF3 inhibitor that exerts anticancer activity against colorectal cancer by modulating the SRSF3 DHCR24 ROS axis and driving apoptosis in CRC cells through the SRSF3 DHCR24 reactive oxygen species (ROS) axis.

Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

DL-Isoleucine exhibits anti-glycation activity in RAW 264.7 cells and exhibits millimolar-level cytotoxicity against SW620, CACO2, SW480, and fibroblast cells.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

CCT070535 inhibits TCF-dependent transcription at the TCF level, displaying GI50 values of 17.6 μM in HT29 (APC mutation), 11.1 μM in HCT116 (oncogenic β-catenin), 11.8 μM in SW480 (APC mutation), and 13.4 μM in SNU475 (Axin mutation) cells.

KHKI-01215 is an effective NUAK2 inhibitor with anticancer activity, inhibiting the proliferation of SW480 cancer cells and inducing apoptosis in SW480 cells. KHKI-01215 is used for cancer research.

SHP2-IN-35 (Compound 3f) functions as an inhibitor of SHP2. It exhibits antiproliferative activity in cancer cell lines RKO, SW480, and CT26, with IC50 values of 5.72 μM, 3.71 μM, and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the expression of cell cycle-related genes, and induces mitochondrial autophagy (autophagy). Within the tumor microenvironment (TME), SHP2-IN-35 suppresses the expression of certain cytokines and chemokines, thereby modulating tumor progression.

5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory properties. It suppresses IL-6, IL-1β, TNF-α, and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. Additionally, 5-LOX-IN-8 decreases the disease activity index in DSS colitis models. This compound is applicable for research in inflammatory bowel disease (IBD).

CLK2/3-IN-1 (Compound 7c) is an orally active inhibitor of CLK2/3, with EC50 values of 5.07 nM and 30.03 nM, respectively. Its inhibitory action is facilitated by hydrogen bonding with Lys193 and Lys186 residues of CLK2/3. This compound effectively inhibits the proliferation of SW480 tumor cells with an IC50 of 163 nM and is applicable for research into CLK-related cancer diseases.

AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonistic activity. It exhibits antiproliferative effects on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells, with EC50 values of 7, 10, 12, 13, 15, and 39 μM, respectively.

PQ1, as an enhancer of gap junction in SW480 human colorectal cancer cells can act by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt/β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg/kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

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.

AMPC is a TFF3 inhibitor with antitumor activity and inhibits tumor growth in vivo. AMPC inhibits cell proliferation and survival in TFF3-positive CMS4 colorectal cancer cells and can be used to study colorectal cancer.

Oxyberberine (8-Oxoberberine) is isolated from the methanol extract of A. mexicana. It has been used to study the SW480 human colon cancer cell line.

Anticancer agent 63 (compound 3h) exhibits significant cytotoxic activity against multiple cancer cell lines, including SW480, HeLa, A549, and MCF-7, with IC50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. It induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression, and also demonstrates antioxidative properties [1].

IMP2-IN-1 (compound 4) is an effective IMP2 inhibitor with an IC50 of 81.3-127.5 μM for IMP2 RNA, reducing IMP2 levels in SW480 cells and significantly inhibiting the activity of both differentiated and undifferentiated Huh7 cells.