sw480

Tubulin inhibitor 32 is an orally active novel microtubule inhibitor with antiproliferative and antitumor activity, inhibits microtubule polymerization, induces apoptosis and cell cycle arrest in G2/M phase.

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

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

Cedrelone is a citrulline analog and a phenazine biosynthesis-like domain protein (PBLD) activator.Cedrelone induces apoptosis in cancer cells.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone has insecticidal activity, inhibiting the growth of arrowhead venom of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus). Cedrelone has insecticidal activity, inhibiting the growth of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus).Cedrelone has antitumor effects and exhibits significant cytotoxicity against cancer cell lines such as -60, SMMC-7721, A-549, MCF-7, and SW480.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone is a very potent inducer of apoptosis, leading to cell cycle arrest.

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.

PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2/M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.

2α,3α,24-Trihydroxyurs-12-en-28-oic acid, a triterpenoid phytoalexin, shows antifungal activity against the fungus mentioned. It also shows in vitro cytotoxic activity against tumor cell lines including PLC,Hep3B,HepG2,HeLa,SW480,MCF-7 and Bel7402.

Ciwujiatone exhibits significant activities against colon cancer cell lines SW480 and SW620.

Musellarin B is cytotoxic toward several of the human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480).

7-Prenyljacareubin shows moderate cytotoxic activity against HL-60, SMMC-7721, A549, MCF-7, and SW480 cell lines.

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

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

Methyl nomilinate, derived from citrus, can modulate cell cycle regulators, thereby inducing cytotoxicity in human colon cancer (SW480) cells in vitro.

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.

XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kinase activation and anchorage-independent growth in NIH 3T3 transformed with v12 H-ras. Since the antiproliferative effect of the compound is not related to the ras phenotype, XR3054 may also have effects on other cell signaling mechanisms.

GPR120-IN-1 is a novel GPR120 inhibitor, showing ~90% inhibitory effects on cell growth with micromolar affinities against SW480.

OSIP-486823（CP248） is a novel and potent microtubule disruptor with affinity for both protein kinase G (PKG) and microtubules.

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

IGUANA-1 free base (STL5-T-0057) acts as a selective ALDH1 B1 inhibitor, demonstrating an IC50 value of 30 nM. It efficaciously inhibits the growth of SW480 cells under both adherent and spheroid conditions, yielding IC50 values of 2.46 μM and 0.39 μM, respectively. This compound is utilized in cancer research.

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.

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.

Eichlerianic acid is a trypanocidal compound with an IC50 value of 10 mg/mL. Eichlerianic acid may have antiviral activity against Herpes simplex virus types I and II in vitro. Eichlerianic acid shows weak cytotoxicity (IC50 6.87 to >40 μM) against human cancer cell (HL-60, SMMC-7721, A-549, MCF-7 and SW480).

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 IC 50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. In particular, Anticancer agent 63 induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression. Additionally, Anticancer agent 63 demonstrates antioxidative properties [1].

Tubulin Inhibitor 21 (compound 6f), a hybrid based on chalcone and melatonin, exhibits potent tubulin inhibition properties. It demonstrates significant cytotoxic activity against SW480 cells (IC 50 =0.26 μM) while showing lesser effects on nonmalignant cells [1].

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

Benitrobenrazide (Hexokinase 2 inhibitor 1) is a hexokinase 2 inhibitor with anticancer and antitumor activity.Benitrobenrazide inhibits the growth of tumors and can be used in cancer research.

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

IMP2-IN-1 (compound 4) is an effective IMP2 inhibitor with an IC50 of 81.3-127.5 μM for IMP2 RNA . IMP2-IN-1 decreased the level of IMP2 in SW480 cells. IMP2-IN-1 significantly inhibited the activity of differentiated and undifferentiated Huh7 cells.