Results for Chemicals & Small Molecules ( 98424 )
Dermatan sulphate sodium, a glycosaminoglycan and thrombin inactivator, exhibits antithrombotic activity by selectively catalyzing the inactivation of thrombin via heparin cofactor II, without interaction with antithrombin III. This compound is noted for its high bioavailability and ability to reduce Bleomycin-induced pulmonary fibrosis damage [1] [2].
Docosapentaenoic acid (DPA), a 22-carbon fatty acid primarily found in fish oil, constitutes a minor fraction of the total unsaturated fatty acids in human serum, with concentrations ranging from 0.1% to 1%, which can increase through dietary supplementation. The all-cis-4,7,10,13,16-DPA variant, also known as Austrian acid, represents a specific isomer of DPA and falls into the omega-6 category, synthesized through the elongation and desaturation of arachidonic acid. In conditions such as fatty acid desaturase syndrome, its levels may decrease, potentially influencing development. Furthermore, conditions like nonalcoholic steatohepatitis, a precursor to hepatocellular carcinoma, are marked by enhanced expression of the hepatic elongase very long fatty acid protein 6 and increased concentrations of very long-chain fatty acids, including all-cis-4,7,10,13,16-DPA.
QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.