erk5in6

Compound 12d is a potent ALK5 inhibitor with an IC50 of 7nM.

1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID targets GRK2.

N-(2-chloro-3-((3,5-dimethyl-4-oxo-3,4-dihydroquinazolin-6-yl)oxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)ethanesulfonamide is a useful organic compound for research in chemistry and life sciences.

1H-benzo[d][1,2,3]triazol-1-yl 8-methoxy-6-nitrophenanthro[3,4-d][1,3]dioxole-5-carboxylate is a useful organic compound for research related to life sciences and the catalog number is T72065.

6-Methyl-5-azacytidine is a potent DNMT inhibitor.

5-Hydroxy-canthin-6-one is a natural product for research related to life sciences. The catalog number is TN3122 and the CAS number is 64118-73-6.

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.

1-Chloro-6-(5-(prop-1-ynyl)thiophen-2-yl)hexa-3,5-diyn-2-ol is a natural product from Laggera pterodonta

Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human) is a peptide utilized as a fluorescence resonance energy transfer (FRET) based substrate for proteolytic activity assays, wherein the cleavage-induced change in fluorescence intensity serves as the measure of enzymatic activity [1].

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.

Eicosapentaenoic acid is an ω-3 polyunsaturated fatty acid that is abundant in marine organisms and fish oils. EPA is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. The biological activity of (±)5(6)-DiHETE has not been documented.

5-Hydroxy-1,7-diphenylhept-6-en-3-one is a natural product for research related to life sciences. The catalog number is TN6357 and the CAS number is 155239-30-8.

5-hydroxy-6-methoxy (S)-Duloxetine is a metabolite of (S)-duloxetine . It is formed from (S)-duloxetine via a 5- or 6-hydroxy duloxetine intermediate, which is formed by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6, and a catechol duloxetine intermediate. 5-hydroxy-6-methoxy (S)-Duloxetine binds to the serotonin (5-HT), norepinephrine, and dopamine transporters with Ki values of 266, 920, and 2,814 nM, respectively.

(±)5(6)-EpETE methyl ester is a derivative of 5(6)-EpETE which is stable enough to ship and handle routinely.(±) 5(6)-EpETE methyl ester is a chemically less reactive derivative of 5(6)-EpETE. The active free acid can be generated from the methyl ester by careful base hydrolysis. Epoxy eicosatetraenoic acids (EpETEs) are the epoxygenase metabolites of EPA. A number of vicinal diol metabolites of EpETEs have been detected in the plasma of patients on marine oil dietary supplementation, while in subjects on a typical western diet these compounds are generally not detected. The specific biologic activity of 5(6)-EpETE and its methyl ester have not been documented.

4-(6-Methyl-4-oxohept-5-en-2-yl)cyclohex-2-en-1-one is a natural product for research related to life sciences. The catalog number is TN2994 and the CAS number is 170380-68-4.

5-n-Heptyl-6-hydroxy-4,7-dioxobenzothiazole acts as a competitive inhibitor at the Qo site of the cytochrome bc1 complex (cytochrome c oxidoreductase) in Saccharomyces cerevisiae [1].

Petunidin-3-O-(6-O-p-coumaryl)-5-O-diglucoside, a natural compound, can be extracted from grapes [1].

4-Chloro-3-methoxy-5-methylphenyl 6-O-(6-deoxy-β-L-mannopyranosyl)-β-D-glucopyranoside (compound 3), a natural anticancer agent extracted from Lilium regale, exhibits potent inhibitory effects on the proliferation of A549 lung cancer cells and holds promise for applications in cancer research [1].

5-Hydroxy-7-methoxy-6-methylflavone is a useful organic compound for research related to life sciences and the catalog number is T131521.

5-Methoxycanthin-6-one displays moderate cytotoxic activity against the human prostate cancer cell PC-3 line, with IC50 values ranging from 13.5-15.4 uM versus doxorubicine with IC50 = 1.5 uM. It also exhibits a clear suppressive effect on the phagocytosi

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.

6-Chloropurine riboside-5'-triphosphate serves as both an inhibitor and an activator in biochemical processes. It inhibits the RNA triphosphatase mRNA-capping enzyme subunit β (Cet1; IC50 = 2 µM for the GTPase activity of the S. cerevisiae enzyme), proving its efficacy against the enzyme responsible for the capping of mRNA molecules. Additionally, it acts as a phosphorylated derivative of 6-chloropurine riboside. This compound also activates the E. coli enzyme aspartate carbamoyltransferase (EC50 = 0.76 mM), demonstrating its versatility in modulating enzyme activities. It is instrumental in the synthesis of cytokinins with anticancer properties and a photoclickable form of ATP, highlighting its applications in biochemical synthesis and potential therapeutic uses.

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).

Ethyl 2-(methylthio)-6-oxo-1,6-dihydropyrimidine-5-carboxylate is a useful organic compound for research related to life sciences. The catalog number is T64927 and the CAS number is 53554-29-3.

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.

Methyl 2-(6-acetyl-5-hydroxy-2,3-dihydrobenzofuran-2-yl)propenoate is a natural product from Vernonia cinerea.

6-Hydroxy-5,7,3',4',5'-pentamethoxyflavone is a natural product for research related to life sciences. The catalog number is TN6355 and the CAS number is 29043-06-9.

(2R,3R,4S,5R)-2-(6-(Benzylamino)-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol is a natural product for research related to life sciences. The catalog number is T65346 and the CAS number is 4294-16-0.

N-[5-[[[3-(6-Amino-4-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide had an IC50 value of 22 nM in a BD2 DEC-Tec assay.

(5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one ((5R)-trans-1,7-diphenyl-5-hydroxy-6-hept) has antioxidant activity.

5-Chloro-6-methoxymellein is a useful organic compound for research related to life sciences. The catalog number is T125466 and the CAS number is 19314-93-3.

5-((4-Bromo-2-chlorophenyl)amino)-4-fluoro-1-methyl-1H-benzo[d]imidazole-6-carboxylic acid is a useful organic compound for research related to life sciences. The catalog number is T66323 and the CAS number is 606144-04-1.

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.

2',4',5'-Trimethoxy-2'',2''-dimethylpyrano[5'',6'':6,7]isoflavone is a natural product for research related to life sciences. The catalog number is TN2708 and the CAS number is 211799-56-3.

1-[(5E)-3-O-[(Bis-di-isopropyl amino)(2-cyanoethoxy) phosphino]-5,6-dideoxy-6-(diethoxyphosphinyl)-2-O-(2-methoxyethyl)-β-D-ribo-hex-5-enofuranosyl]-5-methyluracil is a Nucleoside Phosphoramidite; Nucleoside Derivative - Phosphorus-containing nucleotide; 5'-Modified nucleoside.

Phenanthridinium, 3-amino-8-(3-(3-(((aminoiminomethyl)hydrazono)methyl)phenyl)-1-triazenyl)-5-ethyl-6-phenyl-, chloride, monohydrochloride is a bioactive chemical.

5,6,7,4'-tetrahydroxyisoflavone-6,7-di-O-beta-D-glucopyranoside is a natural product

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.

(2R,3R,4R,5R)-4-(((2S,3R,4R,5S,6R)-3,4-Dihydroxy-6-(hydroxymethyl)-5-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)tetrahydro-2H-pyran-2-yl)oxy)-2,3,5,6-tetrahydroxyhexanal is a natural product for research related to life sciences. The catalog number is T65097 and the CAS number is 33404-34-1.

6-S-(2-Cyanoethyl)-2’-deoxy-5’-O-DMTr--6-thioguanosine 3’-CED phosphoramidite is a useful organic compound for research related to life sciences and the catalog number is TNU1665.

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.

2',3',5'-Tri-O-acetyl-6-chloroguanosine is a Halo-nucleoside.

4-Amino-6-bromo-5-cyano-1-(3-deoxy-3-fluoro-b-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine is a useful organic compound for research related to life sciences and the catalog number is TNU1039.

9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-(5-phenylpyridin-3-yl)purine is a Nucleoside Derivative - Fluoro-modified nucleoside, 6-Modified purine nucleoside, 3'-Modified nucleoside.

2-(((3aR,4S,6R,6aS)-6-((5-Amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol is a useful organic compound for research related to life sciences. The catalog number is T66431 and the CAS number is 376608-74-1.

2-Amino-6-chloro-9-(2-O-acetyl-5-O-benzoyl-3-O-methyl-β-D-ribofuranosyl)-9H-purine is a useful organic compound for research related to life sciences and the catalog number is TNU1594.

(S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor. Its formation occurs through the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6 via a 5- or 6-hydroxy duloxetine intermediate, followed by a catechol duloxetine intermediate. This compound effectively inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) across lipid membranes, with inhibition constants (Kis) of 266, 920, and 2,814 nM, respectively, for human transporters.

1-chloro-6-(5-ethynylthiophen-2-yl)hexa-3,5-diyn-2-ol is a useful organic compound for research related to life sciences and the catalog number is T124214.

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