hct116?cells

TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt β-catenin pathway.

MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity.

Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+ + cells growth inhibitory activity(IC50 = 1.49 μM).

(E)-[6]-Dehydroparadol ((6)-Dehydroparadol), an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator.

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

SSE15206 is a microtubule polymerization inhibitor that overcomes multidrug resistance, causing aberrant mitosis and resulting in G2 M arrest due to incomplete spindle formation in cancer cells.

MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.

TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC).

6-Hydroxycoumarin (6-hydroxychromen-2-one) exhibits cytotoxicity against human HL60, HCT116, COLO205 cells with activity value of 35 uM, 42 uM, 37 respectively. 6-Hydroxycoumarin is a human CA9, CA12 inhibitor.

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2 4 9 and CECR2 (IC50: 0.41 0.29 0.122 0.017 μM), respectively.

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.

IGF2BP1-IN-1 (Compound A11), an inhibitor of IGF2BP1, impedes the associated downstream signaling and demonstrates a high affinity for the IGF2BP1 protein with a dissociation constant (K D) of 2.88 nM. The compound effectively halts the proliferation of cancer cells, as evidenced by an IC50 of 9 nM for A549 cells and 34 nM for HCT116 cells, while also inducing apoptosis in these cells. Moreover, IGF2BP1-IN-1 has been shown to inhibit tumor growth in an A549 xenograft mouse model [1].

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.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1 S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [1].

CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptors in a dose-dependent manner, demonstrating rapid, uniform spread and integration of fluorescence within cell monolayers. In live HCT116 spheroids, it achieves consistent staining throughout, penetrating even the deepest layers. As a fluorescent adenosine receptor probe, CELT-327 is ideal for applications in fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays, serving as an effective alternative to GPCR radiolabeling ligands. Its excitation and emission peaks are at 589 nm and 616 nm, respectively, making it suitable for TR-FRET assays as an acceptor dye, particularly in combination with the CoraFlor1 TR-FRET donor.

MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM. MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

Neoaureothin, a bacterial metabolite found in Streptomyces, is an androgen receptor (AR) antagonist that inhibits dihydrotestosterone (DHT) binding to ARs (IC50 = 13 μM) and DHT-induced prostate-specific antigen expression in LNCaP cells (IC50 = 1.75 nM). It is cytotoxic to A549, HCT116, and HepG2 cells (IC50s = 34.3, 47, and 37.2 μg ml, respectively), exhibits nematocidal activity against the pine wood nematode B. xylophilus (LC50 = 0.84 μg ml), and increases survival of P. densiflora trees inoculated with B. xylophilus.

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound exhibiting antiproliferative activity. It inhibits cancer cell lines HCT116, MCF-7, H460, and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50 values of 0.5 μM, 2 μM, 0.7 μM, and 3.5 μM, respectively.

Carlina oxide is both an AChE inhibitor and an antioxidant, effective in eliminating mosquito larvae (LC50=1.39 μg mL). Furthermore, Carlina oxide exhibits cytotoxicity in vertebrate cells, human dermis, and HCT116 and MDA-MB231 cell lines.

Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-1 is a nutlin-3 analog which contains chlorine substituents at the 3 and 4 positions on two of the phenyl rings rather than a single 4-chloro as seen in nutlin-3. At high concentrations, caylin-1 inhibits the growth of HCT116 cells with an IC50 value of approximately 7 μM, making it about 7-fold less potent than nutlin-3 in the same assay. Interestingly, at concentrations at or below 1 μM, caylin-1 promotes the growth of HCT116 cells approximately 20% compared to untreated cells. The mechanism of the growth promoting properties of caylin-1 have not yet been elucidated.

C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the 20S proteasome in HT-29 and HCT116, but not RIE-1, cells. It reduces tumor growth and increases C16, C18, C20, and C24 ceramide levels in tumor tissue in an HT-29 mouse xenograft model when administered at doses of 1.25, 2.5, and 5 mg/kg for five days. |1. García-Barros, M., Coant, N., Kawamori, T., et al. Role of neutral ceramidase in colon cancer. FASEB J. 30(12), 4159-4171 (2016).

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0/G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

SZ-015268 is a CDK7 inhibitor (IC50: 23.56 nM) that inhibits the proliferation of HCC70 (IC50: 33 nM), OVCAR-3 (IC50: 80.56 nM), HCT116 (IC50: 12.53 nM), and HCC1806 (IC50: 61.55 nM) cells, exhibiting a highly significant anti-tumor effect.

Collismycin A is a bacterial metabolite from *Streptomyces* with antibacterial, antiproliferative, and neuroprotective properties. It exhibits activity against various bacteria (MICs = 6.25-100 μg ml) and fungi (MICs = 12.5-100 μg ml). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s = 0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50 = 56.6 μM) but not MDA-MD-231 breast cancer cells (IC50 > 100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) in a 2:1 ratio, with iron ions inhibiting its antiproliferative effect on HeLa cells, an effect not observed with zinc, manganese, copper, or magnesium ions. Additionally, Collismycin A (1 μM) reduces apoptosis in zebrafish larvae brain regions by 44% in a model of neuronal cell death induced by all-trans retinoic acid.

Tubulin inhibitor 26 (compound 3c) is an indazole derivative and a potent tubulin inhibitor with low nanomolar potency against HepG2, HCT116, SW620, HT29, and A549 cancer cell lines. It inhibits tumor cells in the G2 M phase, induces cell apoptosis, and suppresses tumor growth in vivo without affecting mice body weight [1].

10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).

6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is

AMG-193 (compound 481) acts as an inhibitor of PRMT5, and PRMT5-IN-27 is effective in halting the proliferation of HCT116 cells, exhibiting an IC50 value of 0.13 μM [1].

Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization, inducing concentration-dependent cell cycle arrest at the G2 M phase in HCT116 tumor cells and significantly inhibiting tubulin polymerization with an IC50 of 12.7 μM, showing potential for cancer research [1].

AG-024322 is a potent ATP-competitive inhibitor targeting pan-CDK, effectively inhibiting cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range (1-3 nM).

Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS/ELSD libraries. Bioorg.Med.Chem. 20 4348 PMID:22705020 |Kinder et al (2001) Synthesis and antitumor activity of ester-modified analogues of bengamide B. J.Med.Chem. 44 3692 PMID:11606134

D-threo Sphinganine (d18:0) is a synthetic bioactive sphingolipid and stereoisomer of sphinganine (d18:0) and L-erythro sphinganine (d18:0) . It induces autophagy in HCT116 cells when used at a concentration of 12 μM. D-threo Sphinganine (d18:0) is metabolized via sphinganine N-acyltransferase and sphinganine kinase in vivo in rat liver.

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).

JPS035, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC), specifically HDAC1/2. Its potent activity is associated with an increase in differentially expressed genes and enhanced apoptosis in HCT116 cells [1].

(–)-β-Sesquiphellandrene, a sesquiterpene identified in Z. officinale, exhibits antiviral and anticancer properties. It effectively inhibits rhinovirus IB virus replication in a plaque reduction assay with an IC50 of 0.44 µM. Additionally, at a concentration of 10 µM, it demonstrates cytotoxicity to HCT116 cells.

Anticanceragent 235 (Compound 49) functions as a modulator of the PI3K AKT mTOR signaling pathway, enhancing reactive oxygen species (ROS) production and reducing mitochondrial membrane potential, thereby inhibiting the proliferation of cancer cell lines HCT116, Caco-2, AGS, and SMMC-772 with IC50 values ranging from 0.35 to 26.9 μM. Additionally, it induces apoptosis and causes cell cycle arrest at the G2 M phase in HCT-116 cells.

Trichodermamide B is a JAK STAT3 inhibitor that demonstrates potent antiproliferative activity with an IC50 value of 0.12 μM against HCT116 cells. Furthermore, Trichodermamide B induces cell apoptosis (apoptosis) and exhibits anticancer properties.

8-Acetylverrucarin L (Verrucarin L acetate) is a mycotoxin known for its antitumor and antibacterial properties. It exhibits cytotoxicity against cancer cells HCT116 and A2780S with an IC100 of 9.77 ng mL for both. Moreover, 8-Acetylverrucarin L demonstrates antifungal activity against Saccharomyces cerevisiae, Candida albicans, and Geotrichum candidum.

FL77-24, an analog of FL118 and an apoptosis inducer, exhibits antitumor activity with IC50 values of 99.4 nM in HCT116 cells, 118 nM in HepG2 cells, less than 6.4 nM in both MCF-7 and HeLa cells, and 28.5 nM in A549 cells. It primarily induces cell cycle arrest in the S and G2 M phases [1].

4-(3,4-Difluorobenzo)curcumin (CDF) is a semisynthetic coumarin noted for its antiparasitic and anticancer properties. It effectively reduces the population of Vero cells infected by T. gondii promastigotes and amastigotes, with EC50 values of 0.8 and 0.37 µM, respectively. Furthermore, at concentrations of 4 and 8 µM, CDF enhances the efficacy of 5-fluorouracil and oxaliplatin in inhibiting the formation of both primary and secondary colonospheres in chemoresistant HCT116 cells.

DC 432, a potent peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 value of 54 nM, incorporates a BM30 peptide enhanced by five arginine residues. It effectively reduces the N-terminal methylation level of the regulator of chromosome condensation 1 and SET proteins in HCT116 cells, demonstrating cell permeability.

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.

4-Formylcolchicine, a potent anticancer agent, demonstrates cytotoxicity with IC 50 values of 1.007 µM for A549 cells, 0.128 µM for HT-29 cells, and 0.054 µM for HCT116 cells.

ZLHQ-5f is a dual inhibitor of CDK2 and Topo I, acting on CDK2/CycA2 (IC50: 0.145 μM). ZLHQ-5f has a good safety profile by blocking the cell cycle of HCT116 cells in S phase and inducing apoptosis.

Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-2 is a nutlin-3 analog in which trifluoromethyl groups have been substituted for chlorine on the 2 phenyl rings. At high concentrations, caylin-2 inhibits the growth of HCT116 cells with an IC50 of approximately 8 μM, making it about 10-fold less potent than nutlin-3. Interestingly, at concentrations between 5-100 nM, caylin-2 promotes the growth of HCT116 cells approximately 40% compared to untreated cells. The mechanism of the growth promoting properties of caylin-2 have not yet been elucidated.

Autophagy-IN-1 is a potent inhibitor of autophagy mitophagy that blocks autophagosomal-lysosomal fusion in cancer cells while selectively increasing autophagic flux. It significantly inhibits tumor growth in the HCT116 mouse xenograft tumour model with low toxicity and can be used to study colorectal cancer.