Autres inhibiteurs

<p>GNE-616: a potent, stable, oral Nav1.7 inhibitor; Ki: 0.79 nM, Kd: 0.38 nM; for chronic pain.</p>

O-Desmethyl Midostaurin is the active Midostaurin metabolite via cytochrome P450 liver enzyme metabolism.

<p>PRN694 is a potent, irreversible ITK/RLK inhibitor with IC50s: 0.3/1.4 nM; offers lasting effector cell suppression.</p>

<p>BMS-681 is a CCR2 antagonist blocking chemokine binding, aiding control of inflammatory and neurodegenerative diseases.</p>

<p>FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.</p>

<p>DAD is an ion channel blocker (blocks voltage-gated potassium channels) and is a third generation photoelectric switch that responds to visible light.</p>

<p>Irinotecan Carboxylate Sodium Salt is a DNA topoisomerase inhibitor.</p>

<p>SIK1 activator 1 boosts SIK1 phosphorylation, reduces type 2 diabetes hyperglycemia, and inhibits liver gluconeogenesis.</p>

BMS-986120: Oral, reversible PAR4 antagonist. IC50: 9.5 nM (human), 2.1 nM (monkey). Potent, selective antiplatelet.

FTI 276 TFA targets plasmodium falciparum & humans, inhibits PFT with IC50s: 0.9 nM (parasite) & 0.5 nM (human).

<p>PNU-140457 is a bio-active chemical.</p>

<p>Cicaprost (ZK 96480) is an IP agonist with artery relaxing effects; EC50 is 5.8 nM.</p>

<p>GRPR antagonist-1 targets GRPR, kills specific cancer cells (e.g., PC3, Pan02, HGC-27), and promotes apoptosis by modulating Bcl-2 and Bax.</p>

<p>BMS-520: potent oral S1P1 agonist, effective in rat arthritis and mouse multiple sclerosis model.</p>

<p>Heme Oxygenase-1-IN-2 is a novel inhibitor of heme oxygenase-1 (HO-1), displaying potent antiproliferative activity in vitro, with an IC50 value of 0.95 μM.</p>

<p>SCP1-IN-2: potent, selective SCP1 inhibitor; induces REST degradation, hinders its activity, may study REST-driven glioblastoma growth.</p>

<p>eIF4A3-IN-6 is a potent eIF4A inhibitor, potentially used for treating eIF4A-related diseases like cancer. (US20170145026A1)</p>

Tofogliflozin specifically inhibits SGLT2; IC50s are 2.9 nM (human), 14.9 nM (rat), 6.4 nM (mouse).

Sekdel sequence, as a signal, leads to retention of at least two proteins in the endoplasmic reticulum of animal cells.

<p>LH secretion antagonist 1 is an antagonist of luteinizing hormone secretion with analgesic activity.</p>

<p>XN methyl pyrazole exhibits beneficial effects on diet-induced obesity and enhances energy expenditure in mice fed with a high-fat diet [1].</p>

<p>Rafutrombopag is a thrombopoietin (TPO) agonist.</p>

<p>GNTI TFA is a selective kappa opioid receptor antagonist.</p>

<p>Glyphosate-trimesium is a herbicide.</p>

<p>AD5075 is a bioactive chemical.</p>

<p>Anti-inflammatory agent 23 blocks LPS-induced NO (IC50: 0.449 μM) and binds p65 well.</p>

<p>FCE-24379 is a selective antagonist of vascular serotonin receptors that has been shown to lowers blood pressure in hypertensive rats.</p>

Napsagatran hydrate is a novel and specific inhibitor of thrombin.

<p>Tembotrione is a chemical compound that may reduce the productivity of carrots. It possesses activity that degrades the quality of carrot stems. Additionally, Tembotrione can be used in studies focusing on the overall productivity of carrot cultivation.</p>

<p>DN-F01 exhibits a potent calcium-dependent inhibitory effect on cardiac myofibrillar ATPase activity, with an IC50 of 11 ± 4 nmol/L.</p>

<p>BRD-K25923209 is a novel inhibitor of BAF transcriptional repression.</p>

<p>Vitamin A Propionate, an ester derivative of vitamin A, exhibits varying effects on growth, serum biochemistry, and hematological indices in foal nutrition studies depending on the dosage administered. Both excessively high and low doses lead to adverse impacts. These effects are correlated with the concentrations of vitamin A in the plasma, liver, and kidneys.</p>

<p>YKL-04-085 inhibits viral translation effectively, with strong antiviral action at much lower doses than those affecting host-cell growth.</p>

<p>RIPK1-IN-26 is a potent inhibitor of Receptor-Interacting Serine/Threonine Kinase 1 (RIPK1), exhibiting anti-necrotic properties in cells. This compound demonstrates good metabolic stability and binding specificity in mice. RIPK1-IN-26 holds potential for development as a PET imaging probe and in the research of neurodegenerative diseases.</p>

<p>RIPK1-IN-24 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an IC50 of 1.3 μM. It is utilized in research on inflammatory diseases.</p>

<p>Coleon-U-quinone, a P-gp inhibitor, reduces cancer cell viability and enhances Doxorubicin sensitivity in resistant cells.</p>

<p>CYP1B1-IN-2 (compound 9j) is a highly potent and selective inhibitor of CYP1B1, a cytochrome P450 enzyme. It exhibits an IC50 value of 0.52 nM [1].</p>

<p>Antiviral agent 7 is a peptide-based coating that kills viruses.</p>

<p>Calcipotriol Impurity C is the impurity of Calcipotriol. Calcipotriol is a VDR-like receptors ligand.</p>

<p>GW-311616 is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).</p>

<p>MMP408 acts as an inhibitor of MMP-12.</p>

<p>Oleuroside can protect against mitochondrial dysfunction in models of early Alzheimer's disease and brain ageing.</p>

<p>Damavaricin D exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and fungi.</p>

<p>Balanol is an ATP-competitive Protein Kinase C and Protein Kinase A inhibitor.</p>

<p>ABCA1 inducer 1, a non-lipid inducer of ABCA1, enhances ABCA1 expression in E3/4FAD mice expressing human APOE 3/4, augments the lipidation of apolipoprotein (APOE), and reverses various Alzheimer's disease (AD) phenotypes without increasing triglycerides.</p>

<p>Pyruvate Carboxylase-IN-2, erianin analog, inhibits PC with IC50s of 0.065/0.097 μM in lysate/cell assays, targets HCC.</p>

<p>Cytosaminomycin A is an antibiotic with anticoccidial and antibacterial properties.</p>

<p>EICAR: IMP dehydrogenase inhibitor with anticancer and antiviral properties, failed in leukemia trials, active against various viruses but not SARS.</p>

<p>Epoxyquinomicin B is an antibiotic isolated from Amycolatopsissp. It exhibits inhibitory activity against Micrococcus luteus, Bacillus subtilis, Pasteurella piscicida, and Staphylococcus aureus, with a minimum inhibitory concentration (MIC) of 6.25-12.5 µg/mL. It also shows cytotoxicity in cancer cells L1210, with an IC50 of 16.3 µg/mL. Additionally, Epoxyquinomicin B demonstrates anti-inflammatory effects on collagen-induced arthritis.</p>

<p>Cervicarcin is an antitumor antibiotic (antibiotic) exhibiting strong inhibitory effects on sarcoma 180 and sarcoma NF, while showing weaker activity against sarcoma 37, Ehrlich ascites carcinoma, and Freund leukemia.</p>

<p>Bagremycin B is produced by the bacterium Streptomyces strain Tu 4128. It exhibits weak activity against Gram-positive bacteria, Saccharomyces cerevisiae, and Candida albicans.</p>

<p>Hydroxyakalone is an inhibitor of the enzyme xanthine oxidase (XOD, EC 1.2.3.2) and has an IC50 of 4.6 μM for XOD.</p>

<p>Vps34-IN-3 is a potent, selective, and orally bioavailable inhibitor of VPS34 kinase .</p>

<p>Hetrombopag olamine is a non-peptide thrombopoietin (TPO) receptor agonist with oral activity.</p>

<p>1-Hydroxy-2-nonyn-4-one is an antibiotic with activity against yeasts, filamentous fungi, tumors, and shows weak efficacy against both Gram-positive and Gram-negative bacteria.</p>

<p>AH22921 is an EP4 prostaglandin receptor antagonist with the ability to antagonize the activation of adenylyl cyclase by prostaglandins in CHO cells. It induces a rightward shift in the PGE? concentration-response curve in these cells, functioning as a non-competitive antagonist. AH22921 is selective for the EP4 receptor, inhibiting its activity in CHO cells without affecting the PGE? concentration-response curve in NPE cells that contain the EP2 receptor.</p>

<p>SARS-CoV-2-IN-99 (compound 58) is an inhibitor of the main protease of SARS-CoV-2.</p>

<p>MRS4865 (compound 7a) serves as a chimeric antagonist for the P2Y14 receptor and an agonist for UDP-glucose, offering protection against neuropathic pain.</p>

<p>3'-O-Decarbamoylirumamycin is a 20-membered macrolide antibiotic produced by Streptomyces subflavus subsp. irumaensis. It exhibits inhibitory effects against plant pathogenic fungi, such as Pyricularia oryzae and Sclerotinia.</p>

<p>Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg/L. At a dosage of 10 mg/kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.</p>

<p>2-Hydroxygentamicin B1 is an aminoglycoside antibiotic that exhibits activity against both Gram-positive and Gram-negative bacteria.</p>

<p>PDE5-IN-8 (compound 2) is an inhibitor of PDEs.</p>

<p>Nebramycin IV is an aminoglycoside antibiotic with a broad antimicrobial spectrum, demonstrating significant efficacy against Gram-positive bacteria, Gram-negative bacteria, and mycobacteria.</p>

<p>LY-2979165 is a metabotropic glutamate receptor agonist prodrug.</p>

<p>D-473 is a novel orally active triple reuptake inhibitor targeting dopamine, serotonin and norepinephrine transporters.</p>

<p>Dynemicin Q is an antibiotic that demonstrates potent activity against Gram-positive bacteria.</p>

<p>RK-582: oral spiroindolinone tankyrase inhibitor, halts colon cancer growth in COLO-320DM mouse model.</p>

<p>Nanaomycin D is an antibiotic with antibacterial properties.</p>

<p>Pyrisulfoxin B is an antibiotic produced by the bacterium Streptomyces (BS-75).</p>

<p>Vicanicin is an aryl phenol ether compound found in lichens. It inhibits the expression of Hsp70, modulates intracellular redox-sensitive mechanisms, increases reactive oxygen species (ROS) in cancer cells, alters the Bax/Bcl-2 ratio, activates caspase-3, and induces apoptosis. Vicanicin suppresses cell growth and promotes apoptosis in androgen-sensitive (LNCaP) and androgen-insensitive (DU-145) human prostate cancer cells. It holds potential for prostate cancer research.</p>

<p>Chuangxinmycin is an antibiotic that can be isolated from Actinoplanes tsinanensis CPCC 200056. It exhibits antibacterial activity both in vitro and in vivo, making it useful for research related to infections.</p>

<p>Kerriamycin C exhibits activity against Gram-positive bacteria and also inhibits Ehrlich ascites carcinoma.</p>

<p>VEGFR-2-IN-10 has enhanced antiangiogenic potency against VEGFR2 phosphorylation induced by VEGF with an IC50 value of 0.7 μM and no cytotoxic effects.</p>

<p>UM1 upregulates utrophin, has EC50 of 0.11 μM, useful in DMD research.</p>

<p>Sannamycin K is an aminoglycoside antibiotic with weak antibacterial activity against both Gram-positive and Gram-negative bacteria.</p>

<p>γ-Chloronorvaline exhibits antimicrobial activity against Pseudomonas aeruginosa, Serratia, Klebsiella pneumoniae, and Bacillus subtilis in synthetic media, while it shows no effect on Escherichia coli.</p>

<p>MetRS-IN-1 (Compound 27) is an inhibitor of E. coli methionyl-tRNA synthetase (MetRS) with an IC50 value of 237 nM [1].</p>

<p>Leu-AMS R enantiomer is the R enatiomer of Leu-AMS. Leu-AMS is a potent leucyl-tRNA synthetase (LRS) inhibitor that inhibits the bacteria growth.</p>

<p>α-Prumycin hydrochloride is a carbohydrate antibiotic with antifungal properties and weak antibacterial activity.</p>

<p>Emerin is an antibiotic found in the Aspergillus nidulans strain.</p>

<p>Rezatapopt (PC14586) is a p53 reactivator with antitumor activity for the study of locally advanced or metastatic solid tumors.</p>

<p>Epithienamycin A is a carbapenem antibiotic demonstrating activity against both Gram-positive and Gram-negative bacteria.</p>

<p>CU-2010 is a synthetic compound that reduces blood loss and aids recovery post-cardiac surgery.</p>

<p>Ribocil-C R enantiomer is the R enantiomer of Ribocil-C. Ribocil-C is a highly selective bacterial riboflavin riboswitches inhibitor.</p>

<p>Compound 34e inhibits DENV2/ZIKV proteases; IC50: 0.69 µM (DENV2), 1.04 µM (ZIKV).</p>

<p>FL118 inhibits human survivinion expression and activates tumor suppressor p53 as a MOA in p53 wild-type cancer cells.</p>

<p>SGK1-IN-3: Potent oral inhibitor of SGK1, may target osteoarthritis.</p>

<p>P-gp modulator 2 (Compound 27) is a potent competitive and metabotropic P-glycoprotein (P-gp) modulator.</p>

<p>5-Hydroxy-3,4,7-triphenyl-2,6-benzofurandione is an inhibitor of xanthine oxidase (XO) found in the fungus Peniophora sanguinea.</p>

<p>Oudemansin A is an antibiotic that targets fungi, inhibiting the synthesis of proteins, RNA, and DNA.</p>

<p>5-HT1A/5-HT7 antagonist; 5-HT1A Ki=8 nM, 5-HT7 Ki=451 nM; PDE4B IC50=80.4 μM, PDE7A IC50=151.3 μM; stronger than escitalopram.</p>

<p>PI3Kβ-IN-1 is a selective, orally active PI3Kβ inhibitor (IC50: 2 nM).</p>

<p>Epicorazine A exhibits activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), with a minimum inhibitory concentration (MIC) of 12.5-25 μg/mL. It is also effective against Candida albicans, showing an MIC of 25 μg/mL.</p>

<p>3'-GMP is a nucleotide that can be isolated from the tubers of Helianthus tuberosus L. (Jerusalem artichoke).</p>

<p>PARP7-IN-12, a potent inhibitor targeting PARP7, exhibits an IC50 of 7.836 nM. This compound is applicable in cancer research.</p>

<p>Peridinin is an exceptionally potent and membrane-embedded inhibitor of bilayer lipid peroxidation.</p>

<p>Fistupyrone, an antibiotic, is a microbial metabolite found in Streptomyces (TP-A0569). It has the ability to inhibit infections caused by Alternaria brassicicola in Chinese cabbage.</p>

<p>Darlucin B exhibits both antibacterial and antifungal properties, and it possesses mild cytotoxicity.</p>

<p>β-Carotene-15,15ʹ-epoxide acts as an XIAP antagonist with pro-apoptotic (Apoptosis) and anti-tumor properties, found in the leaves of Spondias mombin. In rat models of DMBA-induced breast cancer, it induces tumor cell apoptosis by binding to the BIR3 domain of the XIAP protein, thereby inhibiting its interaction with caspase-9. Additionally, β-carotene-15,15ʹ-epoxide significantly reduces BCL-2, COX-2, and TNF-α expression in tumor tissue, decreases MDA levels, enhances catalase activity, and modulates biochemical markers in serum such as LDH, ALP, and ALT, indicating its antioxidant, anti-inflammatory, and metabolic protective effects. This compound is useful for researching inflammation-related diseases and tumors such as breast cancer.</p>

C.I. Pigment Red 60 is a bright, scarlet, semi-transparent red pigment.

<p>MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).</p>

<p>3-O-Demethyl-2'-N-glylfortimicin B is a type of aminoglycoside antibiotic.</p>

<p>Saframycin A exhibits antibacterial activity against Gram-positive bacteria and shows weaker effects on Gram-negative bacteria and mycobacteria. Additionally, it inhibits mouse lymphocyte L-1210 cells, with an ID50 of 0.0056 μM.</p>

<p>L 671776 is an inositol monophosphatase inhibitor.</p>

<p>CRV431 is a novel Pan-Cyclophilin Inhibitor, potently inhibiting all cyclophilin isoforms tested - A, B, D, and G (IC50 values ranged from 1-7 nM).</p>