Inhibidores

<p>AZD 3147 inhibits mTORC1 (40.7 nM), mTORC2 (5.75 nM), and PI3Kα/β/δ/γ (912/5495/9333/6310 nM IC50s).</p>

<p>Suzetrigine (VX-548) is an oral NaV1.8 inhibitor with analgesic properties for acute pain research.</p>

<p>WAY-213613 hydrochloride: potent, selective GLT-1/EAAT2 inhibitor (IC50 85 nM); weaker for EAAT1/3; inactive at glutamate receptors; research tool for CNS.</p>

<p>BMS 299897, a sulfonamide γ-secretase inhibitor, inhibits Aβ production with an IC50 of 7 nM in HEK293 cells overexpressing APP.</p>

<p>USP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM).</p>

<p>Eravacycline dihydrochloride (TP-434-046) is a potent and broad-spectrum antibacterial agent against six E. coli (MICs: 0.125-0.25 mg/L).</p>

<p>Lometrexol (LY 264618) is an antifolate that inhibits GARFT, blocks purine synthesis, induces apoptosis, and has anticancer properties.</p>

<p>Gepotidacin mesylate dihydrate (GSK2140944 mesylate dihydrate) is an antibiotic and an inhibitor of bacterial type II topoisomerase.</p>

<p>Milademetan (DS-3032), an MDM2 inhibitor, exhibits antitumor activity, induces G1 cell cycle arrest and apoptosis, and can be used to study solid tumors.</p>

<p>USP5-IN-1, a powerful USP5 deubiquitinase inhibitor, selectively binds with 2.8 μM affinity, blocking USP5's di-ubiquitin cleavage.</p>

<p>Darizmetinib (HRX215) is an MKK4 inhibitor.</p>

<p>AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM.</p>

<p>SJ6986 is a potent, selective and orally active GSPT1/2 degrader. SJ6986 degrades GSPT1 with a DC 50 of 2.1 nM (D max 99%) [1].</p>

<p>AM103 is an effective and selective inhibitor of FLAP (IC50 = 4.2 nM).</p>

<p>Evixapodlin (PD-1/PD-L1-IN 7) is a human PD-1/PD-L1 protein/protein interaction inhibitor (IC50: 0.213).Evixapodlin has anticancer and antiviral activities.</p>

<p>Dazostinag disodium (TAK-676) is a synthetic novel interferon gene (STING) agonist.Cost-effective and quality-assured.</p>

<p>STK-15 is a candidate for use as a fatty acid binding protein 5 (FABP5) inhibitor.</p>

<p>BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin.</p>

<p>Obicetrapib (AMG-899) is an inhibitor of cholesteryl ester transfer protein.</p>

<p>NRX-103094 boosts β-catenin binding to SCFβ-TrCP ligase with EC50 62 nM and Kd 0.6 nM.</p>

<p>Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.</p>

<p>CCF0058981: noncovalent inhibitor for SARS-CoV-2 &amp; -1 proteases; IC50s: 68 nM (SC2) &amp; 19 nM (SC1). Potential COVID-19 research use.</p>

<p>BCL6-IN-3: potent BCL6 inhibitor, 70 nM GI50 in SU-DHL4, affects cell functions, antitumor.</p>

<p>Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist.Cost-effective and quality-assured.</p>

<p>PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.</p>

<p>Tuvusertib (M1774), an oral ATR inhibitor (Ki&lt;1µM), selectively blocks CHK1 phosphorylation, disrupts DNA repair, and induces tumor cell apoptosis.</p>

<p>KI696 is a high-affinity probe that potently inhibits the interaction of Keap1 and NRF2.</p>

<p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</p>

<p>ALOX15-IN-2: Potent ALOX15 inhibitor. IC50: 1.55 μM for LA; 2.79 μM for AA. Stops linoleic/arachidonic acid oxidation.</p>

<p>L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.</p>

<p>MIV-247 is a cathepsin S inhibitor that attenuates mechanically abnormal pain in preclinical neuropathic pain models and can be used to study myocardial injury.</p>

<p>BE1218 is a liver X receptor (LXR) inverse agonist active on LXRα and LXRβ with an IC50 of 9 nM and 7 nM, respectively.</p>

<p>Aleglitazar (R1439) (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively.</p>

<p>Vecabrutinib (SNS-062) is a potent and noncovalent BTK and ITK inhibitor (Kd: 0.3 nM and 2.2 nM, respectively). Vecabrutinib displays an IC50 of 24 nM for ITK.</p>

<p>Zelasudil (RXC007) is a Rho-related (ROCK) kinase inhibitor for the study of idiopathic pulmonary fibrosis and inflammation.</p>

<p>(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) is a reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor, inhibits transport by VMAT2 with 10-fold</p>

<p>HOIPIN-8 sodium is a LUBAC inhibitor for the study of inflammatory and immune diseases.</p>

<p>BLU2864: oral PRKACA inhibitor, IC50=0.3 nM, potential in cancer/poly. kidney disease research.</p>

<p>LLY-283, PRMT5 inhibitor, IC50 22 nM, Kd 6 nM, oral, selective, with antitumor effects.</p>

<p>Tigemonam is a monobactam, a novel orally administered monobactam that protects against gram-negative aerobic bacterial pathogens. Cost-effective and quality-assured.</p>

<p>Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension.</p>

<p>Umibecestat inhibits human and mouse BACE-1 (IC50: 11 nM &amp; 10 nM), potentially for Alzheimer's research.</p>

<p>Dual FAAH/sEH-IN-1 inhibits both sEH (IC50: 9.6 nM) and FAAH (IC50: 7 nM), offering potent anti-inflammatory effects.</p>

<p>AChE/BChE-IN-10 inhibits AChE/BChE (IC50: 0.176/0.47 μM), crosses the blood-brain barrier, and prevents Aβ-aggregation.</p>

<p>Rupintrivirvr (AG7088) is a mimetic peptide inhibitor of rhinovirus (HRV) 3C cysteine protease with antiviral activity for the study of viral infections.</p>

<p>JTK-109 is an inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor and inhibits G1b and G3a subgenomic replicons and recombinant enzymes.</p>

<p>EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 with IC50 of 18 nM in SETD2 biochemical assay and IC50 of 34 nM in a cellular assay.</p>

<p>SB-423562 is a calcium-sensing receptor (CaSR) antagonist and can be used in studies about osteoporosis.</p>

<p>ELOVL1-IN-2 weakly inhibits ELOVL1 enzyme (IC50: 21 μM) and shows moderate potency in HEK293 cells (IC50: 6.7 μM).</p>

<p>NRX-1532 is a small molecule β-catenin:β-TrCP interaction enhancer.</p>

<p>NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd&lt;200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases</p>

<p>O-Propargyl-Puromycin (OP-puro) is a potent protein synthesis inhibitor, a puromycin acetylene analog.</p>

<p>ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.</p>

<p>Moiramide B is an acetyl coenzyme A carboxylase inhibitor with antimicrobial activity, strongly inhibiting Gram-positive bacteria.</p>

<p>GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.</p>

<p>AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor (IC50: 0.42 μM).</p>

<p>BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase ( DNA-PK ) inhibitor ( IC 50 =81 nM) which shows synergistic efficacy in</p>

<p>BRD0639 is a first-in-class PRMT5-substrate interaction inhibitor for PBM-dependent PRMT5 activity studies.</p>

<p>Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.</p>

<p>XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.</p>

<p>CP-4126, a lipophilic pro-drug of Gemcitabine, converts to active form by esterases, allowing oral administration with dose-dependent effects.</p>

<p>CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM.</p>

<p>Rolapitant HCl is a potent NK1 antagonist, non-CYP3A4 interactive, with anti-emetic effects and a Ki of 0.66 nM.</p>

<p>LY3143921 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor with broad in vitro anticancer activity [1].</p>

<p>PD151746: calpain inhibitor, Ki μ-calpain=0.26μM, Ki m-calpain=5.33μM; reduces oxLDL cytotoxicity.</p>

<p>10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata and possesses high anti-cancer properties.</p>

<p>GSK5182 is a racemic mix of (E/Z) isomers, a selective ERRγ inverse agonist (IC50: 79 nM), and induces ROS in liver cancer.</p>

<p>Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral</p>

<p>JAK2-IN-7 selectively inhibits JAK2 (IC50: 3 nM), shows 14-fold selectivity over JAK1/3, FLT3, induces G0/G1 arrest, apoptosis, and has antitumor effects.</p>

<p>ARN19702: orally active, brain-penetrant, selective NAAA inhibitor, IC50 230 nM, broad analgesic profile.</p>

<p>TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4.</p>

<p>SR 11302 is an inhibitor of activator protein-1 (AP-1).</p>

<p>FGI-106 tetrahydrochloride demonstrates potent inhibitory activity across a broad spectrum of viruses, including those causing hemorrhagic fevers such as Ebola</p>

<p>Durlobactam sodium salt (ETX2514) have an IC50 values of 4, 14 and 190 nM against class A KPC-2, class C AmpC and class D OXA-24.Cost-effective and quality-assured.</p>

<p>LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.</p>

<p>FX-11: potent LDHA inhibitor (Ki 8 μM), activates PKM2, reduces ATP, induces oxidative stress/ROS, cell death, shows antitumor effects.</p>

<p>Sebetralstat (KVD900) is an inhibitor of plasma kallikrein and can be used in studies about metabolic diseases.</p>

<p>INCB086550 (PD-1/PD-L1-IN-8) (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 &lt;= 10 nM.</p>

<p>Clorophene (Clorofene) is an antimicrobial agent and can be used in personal care products.</p>

<p>3-Hydroxyhippuric acid is an acyl glycine, which are normally minor metabolites of fatty acids.</p>

<p>4',5'-Dibromofluorescein (Eosinic acid) is a fluorescent dye that can be used as a ligand for protein characterization by spectroscopic analysis.</p>

<p>TEM1/CD248 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 73.6 kDa and the accession number is Q91V98.</p>

<p>TCblR Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with C-6xHis tag. The predicted molecular weight is 32-58 KDa and the accession number is Q9NPF0.</p>

<p>N-Octylmaleimide is an alkylmaleimide, which can inhibit rat liver glucose 6-phosphatase.</p>

<p>(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial the 5-HT1A receptor agonist.</p>

<p>Cysteinylglycine TFA is an endogenous metabolite. It is used in disease diagnosis.</p>

<p>3-Methylcrotonylglycine is an acyl glycine, a normal amino acid metabolite found in urine.</p>

<p>(S)-Rasagiline is rasagiline S-isomer, and is an agent of anti-Parkinson.</p>

<p>L-690330 inhibits human/bovine inositol monophosphatase; Ki: 0.19-0.42 μM. 10x potency vs. mouse/rat IMPase.</p>

<p>TD-106 is a modulator of cereblon (CRBN), and can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.</p>

<p>sodium 4-pentynoate is a alkynylacetate analogue.</p>

<p>(S,S)-Valifenalate is an acylamino acid fungicide and is used to control a wide range of fungi belonging to the class of Oomycetes.</p>

<p>Loviride, a reverse transcriptase inhibitor with IC50 of 0.3 μM, blocks HIV-1/2 and SIV in MT-4 cells.</p>

<p>GAS6 (Growth arrest-specific protein 6) is also known as AXL receptor tyrosine kinase ligand, AXLLG, is a multimodular protein that is up-regulated by a wide variety of cell types in response to growth arrest. Gas6 binds and induces signaling through the receptor tyrosine kinases Axl, Dtk, and Mer whose signaling is implicated in cell growth and survival, cell adhesion and cell migration. GAS6/AXL signaling plays a role in various processes such as endothelial cell survival during acidification by preventing apoptosis, optimal cytokine signaling during human natural killer cell development, hepatic regeneration, gonadotropin-releasing hormone neuron survival and migration, platelet activation, or regulation of thrombotic responses. GAS6 Protein, Human, Recombinant (His) is expressed in HEK293 cells.</p>

<p>Deoxypseudouridine is a nucleotide analog.</p>

<p>Metrizoic acid is an ionic contrast medium. Metrizoic acid displays high osmolality and has a risk of inducing allergic reactions.</p>

<p>3-Acetylcoumarin as a practical ligand for copper-catalyzed CN coupling reactions at room temperature. It has neuroprotective and acaricidal properties.</p>

<p>PRGL493 blocks ACSL4, halts PC3/MDA-MB-231 cancer cell spread, and inhibits MA-10 tumor progesterone. Effective in mouse PC3 tumor model at 0.25 mg/kg.</p>

<p>Anisylacetone (Anisylacetone) is an effective lure for the male melon fly.</p>

<p>3-Methoxyphenylacetic acid belongs to the class of organic compounds known as anisoles. 3-Methoxyphenylacetic acid is slightly soluble (in water) and a weakly acidic compound (based on its pKa).3-Methoxyphenylacetic acid (m-Methoxyphenylacetic acid), a m-hydroxyphenylacetic acid (m-OHPAA) derivative, is a phytotoxin in Rhizoctonia solani. 3-Methoxyphenylacetic acid is used to develop a toxin-mediated bioassay for resistance to rhizoctonia root rot</p>