hct-15

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

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

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.

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.

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.

Mertansine (GMP) refers to the GMP grade reagents of Mertansine. 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.

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.

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

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.

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.

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

3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, and 3beta-O-trans-p-coumaroyltormentic acid are weakly selective for vancomycin-resistant Enterococcus (VRE) compared with eukaryotic cells, with an MIC of 59.4microg mL and a 50% inhibitory concentration (IC50) of 72.0microg mL for monkey kidney epithelial (MA104) cells. A mixture of 3-O-cis-p-coumaroyltormentic acid and 3-O-trans-p-coumaroyltormentic acid shows an inhibitory effect comparable to (-)-epigallocatechin gallate (EGCG) of green tea on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradeca--noylphorbol-13-acetate (TPA).

7-Hydroxycadalene shows cytotoxicity activity against HCT-15 cell line with IC50 18.89 ± 1.2 uM.

Coccinic acid shows inhibitory effects against colorectal carcinoma HCT-15 and oral epithelial cell line KB-3-1.Mixture of coccinic acid and anwuweizonic acid shows significant inhibitory activity against human decidual cells and rat luteal cells in vitro

Schizandriside may have anti-inflammatory effects, it has inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells. It shows significant cytotoxicity against A549, SK-OV-3, SK

Norcepharadione B shows good inhibitory activity against the replication of HSV-1, it also shows antimalarial activity with EC50 values of 7.5mug/ml. Norcepharadione B exhibits significant cytotoxicity against five human tumor cell lines (A-549, SK-OV-3,