hep2

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

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.

Remdesivir (GS-5734) is a nucleoside analog, a broad-spectrum antiviral compound that exerts its activity by inhibiting the RNA-dependent RNA polymerase of viruses. Remdesivir is active against Ebola, SARS, and MERS viruses, and is potentially therapeutic against COVID-19.

PC786 is a potent and selective non-nucleoside RSV L-protein polymerase inhibitor for inhalation therapy of RSV infections, with antiviral activity against RSV-A (IC50=0.09-0.71 nM) and RSV-B (IC 50=1.3-50.6 nM), and the ability to inhibit RSV RNA-dependent RNA polymerase in HEp-2 cells ( RdRp).

Pyrazofurin is a pyrimidine nucleoside analogue that potently inhibits cell proliferation and DNA synthesis by targeting UMP synthase, while also acting as a highly sensitive orotate-phosphoribosyltransferase inhibitor with IC50 values ranging from 0.06 to 0.37 μM in Hep-2, HNSCC-14B, and HNSCC-14C cell lines, supporting the use of Pyrazofurin as a mechanistic probe for nucleotide biosynthesis inhibition and antiproliferative research.

Biguanidinium-porphyrin free TFA is a mitochondrial-targeting photosensitiser exhibiting low dark toxicity towards human hepatocellular carcinoma HEp2 cells (IC50=8.2 mM, 1 J/cm²).

EP2 receptor antagonist-3 is a selective antagonist of the EP2 receptor, with an IC50 of 8 nM determined in the hEP2 SPA assay and an IC50 of 50 nM in the hEP2 cAMP assay. It enhances macrophage-mediated clearance of Amyloid-β plaques. In CD-1 mice, it shows moderate clearance and good exposure, and exhibits good central nervous system (CNS) exposure in both mice and rats. EP2 receptor antagonist-3 is applicable for research in Alzheimer's disease.

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM, exhibiting antimalarial activity by inducing developmental arrest of malaria parasites at the schizont stage[1][2].

TG8-260 is a second-generation EP2 antagonist developed to mitigate pathology in inflammatory-driven central and peripheral nervous system disorders. In a rat model, TG8-260 reduced neuroinflammation and gliosis in the hippocampal region following pilocarpine-induced status epilepticus. Pharmacokinetic data for TG8-260 reveal a plasma half-life of 2.14 hours and an oral bioavailability of 77.3%. Furthermore, TG8-260 acts as a potent inhibitor of CYP450 and demonstrates antagonistic activity by inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglial cells, making it suitable for research on anti-inflammatory pathways in animal models of peripheral inflammatory diseases.

Ivangustin, a sesquiterpene lactone derived from the medicinal plant Inula britannica, exhibits significant cytotoxicity against HEp2, SGC-7901 and HCT116 human cancer cell lines.

13(E)-Labd-13-ene-8alpha,15-diol shows antiviral and anticancer activity, it shows strong anti-HRV2 and HRV3 activity with a 50% inhibitory concentration (IC50) of 2.68 and 0.87 microg/mL,respectively; it also exhibits antilung and antilaryngeal cancer ac

Piscidinol A is toxic against the 4T1 and HEp2 cancer cell lines, the IC50 of 8.0 ± 0.03 and 8.4 ± 0.01 uM, respectively. It can inhibit NO production in mouse peritoneal macrophages with inhibitory ratios ranging from 39.8±7.7 to 68.2±4.5%.

4-[2-(3,5-Dimethoxyphenyl)ethyl]phenyl 6-O-(6-deoxy-α-L-mannopyranosyl)-β-D-glucopyranoside showed cytotoxic activities to Hela and hep2 cell lines.