sw480

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.

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

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

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.

MG-101 (Calpain inhibitor I) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

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.

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.

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.

pan-KRAS-IN-8 (Compound 38) is an inhibitor of the human tumor mutated gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.07 nM and 0.18 nM, respectively.

Pan-KRAS-IN-10 (Compound 58) acts as an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells, specifically AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.7 and 0.24 nM, respectively.

pan-KRAS-IN-7 (Compound 25) is an inhibitor of the human tumorigenic mutant gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with an IC50 of 0.35 nM and 0.51 nM, respectively.

Pan-KRAS-IN-8 (Compound 52) is an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 values of 0.24 nM and 0.30 nM, 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.