hct-15

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.

ZINC05007751 is an effective inhibitor of NIMA-related kinase NEK6 (IC50 = 3.4 μM). ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity observed against NEK2, NEK7, and NEK9.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.

Gallic acid (Benzoic acid) is found in almost all plants. Plants known for their high gallic acid content include gallnuts,grapes,tea,hops and oak bark.

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.

Antiproliferative agent-15 is a reagent with anticancer activity. Antiproliferative agent-15 showed antiproliferative activity against human colon cancer (HCT116 and HCT15) and brain cancer (LN-229 and GBM-10).

Kinetin riboside (N6-Furfuryladenosine) can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells(IC50 of 2.5 μM)

Osajin is an isoflavonoid natural product isolated from the fruits of Maclura pomifera. It belongs to flavonoid derivatives, and studies have reported that it exhibits multiple biological activities, including anticancer, antioxidant, and anti-inflammatory effects.

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

A-259745 is an orally active antimitotic agent that binds to the colchicine site on tubulin. It exhibits potent in vitro cytotoxic activity against both multidrug-resistant and non-multidrug-resistant cancer cell lines, with ED50 values of 0.018 μM for HCT-15 and 0.028 μM for NCI-H460 cells. A-259745 inhibits tubulin polymerization, disrupting the dynamic equilibrium of the mitotic spindle, causing dividing cells to arrest in the metaphase-anaphase transition, which subsequently induces apoptosis (apoptosis). In mouse tumor models, A-259745 demonstrates dose-dependent antitumor efficacy and is useful for cancer research.

CC-11 is an orally bioavailable small molecule drug conjugate (SMDC) that links a PI3K/mTOR inhibitor to an extracellular heat shock protein 90 (EHSP90) targeting ligand via a cleavable linker. It exhibits strong binding activity to HSP90 (IC50 = 15 nM) and inhibits PI3Kα kinase activity (IC50 = 0.54 nM). CC-11 shows antiproliferative effects against colon cancer cells and demonstrates significant efficacy in the HCT-116 xenograft model. It is applicable in colon cancer research.

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. It has IC50 values of 0.68, 1.02, 1.03, 8.03, and 15 nM for PI3Kα/β/γ/δ and mTOR, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines such as HCT-116 (IC50= 0.38 μM) and HT-29 (IC50= 1.70 μM). This compound is applicable in colorectal cancer (CRC) research.

TAK1-IN-2 is a potent and selective TAK1 inhibitor with an IC50 of greater than 2 nM [1].

RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells [1].

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.

Angiogenesis Inhibitor 3 (Compound 8) is a potent substance that effectively inhibits the growth of HUVEC and HCT-15 cells, demonstrating IC50 values of 1.00 and 0.71 μM, respectively. It not only induces apoptosis in these cells but also exhibits significant anticancer activity by suppressing cancer cell invasion. Furthermore, this compound successfully inhibits angiogenesis in zebrafish embryos [1].

WES-1 (Compound 8g), a carbonic anhydrase IX inhibitor (Ki: 55.9 μM), exhibits broad-spectrum antiproliferative activity against various cancer cell lines, including leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI-H460), colon cancer (HCT 116 and HCT-15), and melanoma (LOX IMVI) [1].

SLU-10482, an antiparasitic agent, effectively reduces C. parvum parasitic load in HCT-8 cells with an EC50 value of 0.07 µM. It exhibits lower affinity for human ether-a-go-go (hERG; Kd = 43 µM) compared to its counterpart, SLU-2633. When administered in vivo at dosages of 5 and 15 mg/kg twice daily, SLU-10482 significantly decreases fecal oocyst counts in mice infected with C. parvum.

C3N-Dbn-Trp2 is an inhibitor of the ATP-binding cassette transporter ABCB1. It inhibits the efflux of Rhodamine 123 mediated by ABCB1 in HEK293T and HCT-15 cells, with IC50 values of 5.9 µM and 2.2 µM, respectively. Additionally, C3N-Dbn-Trp2 inhibits the efflux of Doxorubicin, thereby enhancing the cytotoxicity of Doxorubicin in cells expressing ABCB1.

hDHODH-IN-15 (Compound H19) acts as an inhibitor of human dihydroorotate dehydrogenase (hDHODH), demonstrating an IC50 of 0.21 µM. It exhibits cytotoxic effects in cancer cells such as NCI-H226, HCT-116, and MDA-MB-231, with IC50 values ranging from 0.95 to 2.81 µM. Furthermore, hDHODH-IN-15 induces ferroptosis in HCT-116 cells and shows antitumor activity.

Antitumor agent-182 (Compound 12a) reduces mitochondrial membrane potential (MMP) and elevates levels of reactive oxygen species (ROS). It impedes the cell cycle during the G0/G1 phase and induces apoptosis in HeLa cells. Furthermore, Antitumor agent-182 inhibits the proliferation of HeLa, PC-3, and HCT-15 cells with IC50 values of 8.83, 10.07, and 7.84 μM, respectively.

Coccinine ((-)-Coccinine) is a weak inhibitor of SERT with an IC50 of 196.3 μM and a Ki of 106.8 μM, and P-gp with an IC50 of 0.96 mM. It demonstrates significant antitumor activity against various cancer cell lines, including breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Additionally, Coccinine is applicable in research involving tumors and neurological disorders.

Cnidicin has anti-allergic and anti-inflammatory activity, it inhibits the degranulation of mast cell and the NO generation in RAW 264.7 cells(IC50 value, 7.5 microM). Cnidicin exhibits a significant inhibition on the proliferation of cultured human tumor