Organometallic Ligands

HS-1371 is a selective chemical inhibitor targeting specific enzymes, which is derived from synthetic organic compounds with a high affinity for its target proteins. It functions by selectively binding to the active site of the enzyme, inhibiting its activity and subsequently influencing downstream signaling pathways within the cell. This mode of action allows researchers to dissect complex biochemical pathways and assess the impact of enzyme inhibition on cellular functions.

Temozolomide is an imidazotetrazine alkylating agent. It has anti-tumor activity against a broad spectrum of tumors, such as leukemias, lymphomas and solid tumors. Temozolomide induces G2/M arrest, preventing cells from entering mitosis and, therefore, apoptosis. As a drug resistance-modifying agent it is used for studying drug resistance mechanisms in glioblastoma cell lines.

AP 1903 is a synthetic small molecule, which acts as a dimerizer ligand. It is derived from the modification of the macrolide antibiotic rapamycin to remove its immunosuppressive effects, thus enabling targeted control of cellular processes. The mode of action involves binding to engineered receptors on the cell surface that contain drug-dependent domains. This binding triggers the dimerization of these receptors, leading to downstream signaling and subsequent cellular responses.

Hispolon is a naturally occurring polyketide compound, which is derived from the mushroom Phellinus linteus, commonly found in Asia. This compound is known for its diverse biological activities, primarily functioning as an antioxidant, anti-inflammatory, and antitumor agent. The mode of action of hispolon involves the modulation of multiple cellular pathways. It has been shown to induce apoptosis in cancer cells by triggering intrinsic and extrinsic apoptotic pathways. Additionally, hispolon exhibits the ability to inhibit the NF-κB pathway, subsequently decreasing the expression of pro-inflammatory cytokines and leading to an anti-inflammatory effect.

Inhibitor of 5-lipoxygenase activating protein_x000D_

Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic

Modulator of S1P receptor

Specific inhibitor of the phosphoinositide 3-kinase (PI3K) alpha subunit with IC50 of 32 nM. In heart muscle it negatively regulates hypertrophic growth, causes increase in late sodium current and leads to arrhythmias. In tumours it inhibits the p110α subunit of PI3K and blocks growth factor signalling resulting in reduced tumour growth.

Piracetam analog; AMPA receptor allosteric modulator

Diphenidol is an antiemetic agent used for the treatment and prevention of nausea and vomiting associated with various conditions. Its mechanism of action is not well known but it is thought to diminish vestibular stimulation and depress labyrinthine function.

17:0-20:4Pi (4) P is a synthetic phosphoinositide, which is a type of phospholipid. It is typically sourced from laboratory synthesis, often incorporating stable isotopes or specific fatty acid chains to mimic natural compounds found in cell membranes. This product functions primarily as a probe in biochemical experiments, particularly for studying lipid signaling pathways within cells.

Fexofenadine is a selective histamine-1 receptor antagonist that is used to treat the symptoms of seasonal allergies. It does not cross the blood-brain barrier and carries little-to-no activity at off targets. This drug binds to the inactive form of the H1 receptor and inhibits its activation and downstream effects.

Agonist of β3-adrenoreceptors with thermogenic properties and potential to control diet-induced obesity. The compound reversed obesity in adult rats and was effective even in animals that continued to feed on high-fat food. It caused the enlarged white adipocytes to shrink and triggered remodelling of the white adipose tissue.

Potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 2.4 nM. Its anti-inflammatory activity was examined in a mouse model for acute colitis. The compound protected from intestinal inflammation by prevention of infiltration of CD19+ B-cells into the lamina propria of colonic epithelium and attenuated neutrophil activation. Its broad anti-inflammatory response involved decrease in 24 inflammatory chemokines and cytokines. Also, it is a potent inhibitor of cell proliferation in pancreatic cancer cell lines.

Droperidol is a butyrophenone derivative, which is an antipsychotic agent and antiemetic medication, sourced from synthetic chemical processes. Its mode of action involves antagonism of dopamine D2 receptors in the central nervous system, particularly in the chemoreceptor trigger zone of the brain, and it also possesses some alpha-adrenergic blocking properties.

Halogenated derivative of febrifugine; coccidiostat

Dipeptidyl peptidase 4 (DPP4) inhibitor

TIC10 is a small molecule, which is sourced from a synthetic chemical library, with a novel mode of action that involves the induction of the tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) pathway. This pathway is distinguished by its ability to selectively trigger apoptosis in cancer cells while sparing normal cells. TIC10 effectively crosses the blood-brain barrier, a feature that enhances its potential application in treating brain-related malignancies.

Inhibits urate anion exchanger 1 (URAT1); therapeutic use in gout