1-(3',5'-dimethoxy)phenyl-2-[4''-O-β-D-glucopyranosyl (6→1)-O-α-L-rhamnopyranosyl]phenylethane showed cytotoxic activities to Hela and hep2 cell lines.
5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM.
CDK4 6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4 Cyclin D1 and CDK6 Cyclin D3, respectively (WO2019207463A1, example A93).
2-Amino-6-chloropurine -9-beta-D-(2'-deoxy-3',5'-di-O-benzoyl-2'-fluoro)arabinoriboside is a Fluoro-modified nucleoside; Halo-nucleoside; Arabino-nucleoside.
5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50 = 0.54 μM), and Cav3.3 and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5(6)-EET is provided as a mixture of the free acid and lactone.
Phenanthridinium, 3-amino-8-(3-(3-(((aminoiminomethyl)hydrazono)methyl)phenyl)-1-triazenyl)-5-ethyl-6-phenyl-, chloride, monohydrochloride is a bioactive chemical.
9-(2'-O-Acetyl-5'-O-benzoyl-3'-deoxy-beta-D-ribofuranosyl)-6-chloropurine is a Nucleoside Derivative - 3'-Deoxy nucleoside, Halo-nucleoside; Scaffold and Template.
2-Amino-6-chloro-9-(3-deoxy-2-O-acetyl-5-O-benzoyl-beta-D-ribofuanosyl)-9H-purine is a Nucleoside Derivative - 3'-Deoxy nucleoside, Halo-nucleoside; Scaffold and Template.
2,4,6-Trichlorol-3-methyl-5-methoxy-phenol 1-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside is a chlorophenyl glycoside that is commonly found in the bulbs of Lilium brownie var. viridulum. This compound has been observed to exhibit a weak inhibition of NO production in LPS-stimulated RAW 264.7 cells.
5(S),6(R)-11-trans DiHETE is a C-11 double bond isomer of 5(S),6(R)-DiHETE that is formed by the enzymatic isomerization of 5(S),6(R)-DiHETE by a membrane bound factor. 5(S),6(R)-11-trans DiHETE has been found in rat kidney homogenates and is potentially formed by the epoxide hydrolase pathway in this tissue. The isomerase activity responsible for the conversion of leukotriene B4 (LTB4) to 6-trans LTB4 in rat kidney homogenates has also been implicated in its formation. 5(S),6(R)-11-trans DiHETE is not a substrate for soybean lipoxygenase. The biological activity of 5(S),6(R)-11-trans DiHETE has not been reported.
Potent and selective cereblon degrader (DC50 = 1.5 nM). Induces complete degradation of cereblon in MM1S cells. Comprises a cereblon E3 ligase ligand joined by a linker to a ligand for the E3 ligase VHL. Cell-permeable. Steinebach et al (2019) PROTAC-mediated crosstalk between E3 ligases. Chem.Commun.(Camb) 55 1821 PMID:30672516