• H 89 dihydrochloride is a cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase. (adooq.com)
  • NH125 is a selective eEF-2 kinase inhibitor. (adooq.com)
  • Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC 50 of 6.7 nM for AChE activity. (medchemexpress.com)
  • 3, 9 Therefore, H-8 represents a promising lead structure for the development of novel PKN3 selective inhibitors and is easy to obtain in a one-step synthesis for an undergraduate student. (openlabnotebooks.org)
  • Identification of novel, selective, and stable inhibitors of class II histone deacetylases. (irbm.com)
  • Nevertheless, the majority of current TRPM8 inhibitors demonstrated HCL Salt also agonistic/antagonistic properties towards additional receptors and also have unwanted effects that justify the necessity for new, even more selective substances25, 26. (conferencedequebec.org)
  • 2019 ) Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors. (academictree.org)
  • AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. (adooq.com)
  • PKA inhibitor fragment (6-22) amide is a synthetic peptide that acts as a protein kinase inhibitor. (adooq.com)
  • PKI 14-22 amide, myristoylated is a useful heat stable cAMP-dependent protein kinase inhibitor. (adooq.com)
  • cGMP Dependent Kinase Inhibitor Peptid is a specific cGKI (cyclic GMP-dependent protein kinase) inhibitor. (adooq.com)
  • Fasudil hydrochloride is a cyclic nucleotide-dependent Rho-associated kinase inhibitor. (cellgs.com)
  • Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. (justia.com)
  • In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. (justia.com)
  • Although some potent PKN3 inhibitors (Figure 1) having been disclosed in the literature, 3 structure activity relationships of these compounds and PKN3, to our knowledge, have not been explored. (openlabnotebooks.org)
  • To explore structure activity relationships, we synthesized a set of compounds with isoquinoline scaffold. (openlabnotebooks.org)
  • In vitro activators, metyrapone, and isoquinoline, stimulated the microsomal activity, but the former had no such effect on the purified enzyme in case of this substrate. (elsevierpure.com)
  • We confirmed that isoquinoline alkaloid is structurally varied from the existing direct AMPK activators. (oncotarget.com)
  • Neuraminidase inhibitors (NAIs) are a class of drugs which block the neuraminidase enzyme. (wikipedia.org)
  • Quinapril hydrochloride and hydrochlorothiazide is a fixed-combination tablet that combines an angiotensin-converting enzyme (ACE) inhibitor, quinapril hydrochloride, and a thiazide diuretic, hydrochlorothiazide. (nih.gov)
  • During her PhD at the Ruđer Bo ković Institute (Zagreb, Croatia), she was engaged in computational modeling of enzymatic reactions, mainly inhibition of MAO B enzyme by propargylamine inhibitors. (efmc-ymcs.org)
  • 2021 ) The endocannabinoid 2-arachidonoylglycerol and dual ABHD6/MAGL enzyme inhibitors display neuroprotective and anti-inflammatory actions in the in vivo retinal model of AMPA excitotoxicity. (academictree.org)
  • Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. (adooq.com)
  • HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively). (adooq.com)
  • AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, little activity outside the AGC kinase family. (adooq.com)
  • CCG215022 is a potent GRK2 and GRK5 inhibitor. (adooq.com)
  • α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC 50 of 9 μM. (medchemexpress.com)
  • Galanthamine is a potent acetylcholinesterase ( AChE ) inhibitor with an IC 50 of 500 nM. (medchemexpress.com)
  • Donepezil is a specific and potent AChE inhibitor. (medchemexpress.com)
  • 11 , 19a - c , and 19f were weakly active at 10 mM indicating that further chemical optimization needs to be performed to obtain potent PKN3 inhibitors. (openlabnotebooks.org)
  • 2021 ) Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors. (academictree.org)
  • Since alpha-synuclein (alpha-Syn) aggregation is a major hallmark in the pathogenesis of PD, we aimed to evaluate the anti-aggregative potential of pharmacological ROCK inhibition using the isoquinoline derivative Fasudil, a small molecule inhibitor already approved for clinical use in humans. (mpg.de)
  • Laninamivir Oseltamivir (Tamiflu) Peramivir (Rapivab) Zanamivir (Relenza) Cyanidin-3-sambubioside (extracted from black elderberry) Coptisine[citation needed] Berberine Discovery and development of neuraminidase inhibitors Smith BJ, McKimm-Breshkin JL, McDonald M, Fernley RT, Varghese JN, Colman PM (May 2002). (wikipedia.org)
  • We chose five isoquinoline alkaloids (berberine, coptisine, palmatine, jateorrhizine, epiberberine) and one aporphine alkaloid (magnoflorine) of Rhizoma coptidis as research goals (Fig. 1 ). (springer.com)
  • An efficient diastereoselective route is developed to get access to novel spiropyrrolo[1,2-a]isoquinoline-oxindole skeletons by a one-potthree-component [3 + 2] cycloaddition reaction of (Z)-5-arylidene-1,3-thiazolidine-2,4-diones, isatin derivatives, and 1,2,3,4-tetrahydroisoquinoline (THIQ). (ubfc.fr)
  • Assays for isoquinoline or quinolizidine alkaloids are not routinely available. (medscape.com)
  • Proven by the use of apoptosis-resistant cellular models and autophagic assays, such isoquinoline alkaloid-induced cytotoxic effect involves energy- and autophagy-related gene 7 (Atg7)-dependent autophagy that resulted from direct activation of AMP activated protein kinase (AMPK). (oncotarget.com)
  • TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. (medchemexpress.com)
  • Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase ( AChE ) inhibitor. (medchemexpress.com)
  • Nowadays only acetylcholinesterase inhibitors are being used for the treatment of AD, they can relieve symptoms of AD, but can't stop progression of the disease. (cuni.cz)
  • Utilizing three different synthesis routes isoquinoline amides and sulfonamides were synthesized (Figure 3, A-C). (openlabnotebooks.org)
  • Synthesis of new isoquinolines as potential PKN3 inhibitors. (openlabnotebooks.org)
  • In a sustained search for novel α-amylase inhibitors for the treatment of type 2 diabetes mellitus (T2DM), we report herein the synthesis of a series of nineteen novel rhodanine-fused spiro[pyrrolidine-2,3′-oxindoles]. (ubfc.fr)
  • In this review, we provide a summary of STING inhibitors, classified by different structural skeletons, reported in patents published from 2019 to July 2022. (eurekaselect.com)
  • 2019 ) Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology. (academictree.org)
  • A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM). (adooq.com)
  • A related isoquinoline derivative, PF-05105679, demonstrated clinical effectiveness HCL Salt in cold-related discomfort in human beings23, 24. (conferencedequebec.org)
  • CHEMBRDG-BB 4002849;Isoquinolin-5-YlBoronic acid;Isoquinolin-4-YlBoronic acid;Isoquinoline-4-boronic acid;4-IsoquinolinYLboronic acid;AKOS BRN-0121;AK. (loto371.com)
  • A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively. (adooq.com)
  • Berberine is a compound found in the protoberberine group of isoquinoline alkaloids, and is considered the major active component present in several plant species. (restorativemedicine.org)
  • The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors. (justia.com)
  • 4.1.5 Additional Hsp90 N-Domain Inhibitors Three additional Hsp90 inhibitors have came into clinical trial. (forgetmenotinitiative.org)
  • Rp-cAMPS is a cell-permeable and reversible inhibitor of PKA (protein kinase A) (Ki = 11 uM). (adooq.com)
  • Unlike the M2 inhibitors, which work only against the influenza A virus, NAIs act against both influenza A and influenza B. The NAIs oseltamivir and zanamivir were approved in the US and Europe for treatment and prevention of influenza A and B. Peramivir acts by strongly binding to the neuraminidase of the influenza viruses and inhibits activation of neuraminidase much longer than oseltamivir or zanamivir. (wikipedia.org)
  • TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. (medchemexpress.com)
  • Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. (irbm.com)
  • Four substances which belong to isoquinoline alkaloids: stylopine, tetrahydropalmatine, canadine and scoulerine were tested. (cuni.cz)
  • Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors. (irbm.com)
  • Quinolizidine and isoquinoline are a widely distributed, heterogeneous group of alkaloids with members of each group having known toxicity to humans and domestic animals. (medscape.com)
  • Lamellarins isolated from marine invertebrates [6] are inhibitors for HIV-1 integrase and also have immuno modulatory activity [7,8] . (beilstein-journals.org)
  • The principal metabolite of quinapril, quinaprilat, is an inhibitor of ACE activity in human subjects and animals. (nih.gov)
  • Pyrimidine deriviatives are ubiquination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders. (justia.com)
  • Under the supervision of David Drewry, Guillermo's project aimed at synthesizing small molecules that should explore the SAR around the PKN3 inhibitor H-8. (openlabnotebooks.org)
  • One approach to mitigate these drawbacks would be the development of a small molecule PKN3 inhibitor. (openlabnotebooks.org)
  • She is currently interested on identifying small molecules inhibitors of Lactate dehydrogenases (LDHs), proteins involved in cancer metabolic adaptations. (efmc-ymcs.org)
  • Two kinds of [3 + 2] cycloaddition intermediates generated from the three-component reactions of 2-bromobenzaldehydes and maleimides with amino esters or amino acids were used for a one-pot N -allylation and intramolecular Heck reactions to form pyrrolidinedione-fused hexahydropyrrolo[2,1- a ]isoquinolines. (beilstein-journals.org)
  • However, after the pandemic caused by H1N1 in 2009, the effectiveness of early treatment with neuraminidase inhibitors in reducing serious cases and deaths was reported in various countries. (wikipedia.org)
  • Rho kinase (ROCK) inhibitors in the management of corneal endothelial disease. (jefferson.edu)
  • However, the development of STING inhibitors is still in its infancy. (eurekaselect.com)
  • Isoquinoline sulfonamide H-8 (Figure 2), previously reported as a PKA/PKG 8 inhibitor, shows a K i value of 10 nM for full-length human PKN3 in an off-chip mobility shift assay. (openlabnotebooks.org)
  • This graph shows the total number of publications written about "Isoquinolines" by people in this website by year, and whether "Isoquinolines" was a major or minor topic of these publications. (jefferson.edu)
  • In conclusion, isoquinoline alkaloid is a new class of compound that induce autophagic cell death in drug-resistant fibroblasts or cancers by exhibiting its direct activation on AMPK. (oncotarget.com)
  • Substrates or inhibitors which are not primarily found or designed to be ligand of any alpha/beta hydrolases. (inrae.fr)
  • Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C. Antimicrob Agents Chemother. (jefferson.edu)
  • The effects of histamine were reversed by a protein kinase A (PKA) inhibitor, N-[2-(4-bromocinnamylamino) ethyl]-5-isoquinoline (H89), and mimicked by a dibutyryl cAMP and an adenylate cyclase activator, forskolin. (elsevierpure.com)
  • Below are the most recent publications written about "Isoquinolines" by people in Profiles. (jefferson.edu)