SelectiveKinase inhibitorCompoundsActivatorsEnzymeProtein kinasesPotentInhibitionCoptisineDerivativesAssaysAcetylcholinesteraseSynthesis2019HydrochlorideDerivativeAcidIC50BerberineEGFRClinicalReversibleInhibitsNovel oralBelongBiological evaluationHumansActivitySmallReactionsEffectivenessROCKDevelopmentShowsClassFoundStudiesTargetCAMPPublications
Selective7
- 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)
Kinase inhibitor5
- 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)
Compounds4
- 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)
Activators2
- 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)
Enzyme4
- 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)
Protein kinases2
- 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)
Potent7
- 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)
Inhibition1
- 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)
Coptisine2
- 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)
Derivatives1
- 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)
Assays2
- 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)
Acetylcholinesterase3
- 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)
Synthesis3
- 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)
20192
- 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)
Hydrochloride1
- 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)
Derivative1
- A related isoquinoline derivative, PF-05105679, demonstrated clinical effectiveness HCL Salt in cold-related discomfort in human beings23, 24. (conferencedequebec.org)
Acid1
- CHEMBRDG-BB 4002849;Isoquinolin-5-YlBoronic acid;Isoquinolin-4-YlBoronic acid;Isoquinoline-4-boronic acid;4-IsoquinolinYLboronic acid;AKOS BRN-0121;AK. (loto371.com)
IC501
- 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)
Berberine1
- 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)
EGFR1
- 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)
Clinical1
- 4.1.5 Additional Hsp90 N-Domain Inhibitors Three additional Hsp90 inhibitors have came into clinical trial. (forgetmenotinitiative.org)
Reversible1
- Rp-cAMPS is a cell-permeable and reversible inhibitor of PKA (protein kinase A) (Ki = 11 uM). (adooq.com)
Inhibits2
- 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)
Novel oral1
- 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)
Belong1
- Four substances which belong to isoquinoline alkaloids: stylopine, tetrahydropalmatine, canadine and scoulerine were tested. (cuni.cz)
Biological evaluation1
- 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)
Humans1
- 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)
Activity3
- 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)
Small3
- 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)
Reactions1
- 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)
Effectiveness1
- 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)
ROCK1
- Rho kinase (ROCK) inhibitors in the management of corneal endothelial disease. (jefferson.edu)
Development1
- However, the development of STING inhibitors is still in its infancy. (eurekaselect.com)
Shows2
- 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)
Class1
- 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)
Found1
- Substrates or inhibitors which are not primarily found or designed to be ligand of any alpha/beta hydrolases. (inrae.fr)
Studies1
- 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)
Target1
- Hsp90 C-Domain Inhibitors All medical Hsp90 inhibitors target the N-terminal ATP binding site. (forgetmenotinitiative.org)
CAMP1
- 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)
Publications1
- Below are the most recent publications written about "Isoquinolines" by people in Profiles. (jefferson.edu)