Inibitori

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

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

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

<p>SDZ 220-040 是一种选择性哺乳动物 NMDA 受体拮抗剂，可诱导根系生长的部分无重力模式 。</p>

<p>O-Propargyl-Puromycin (OP-puro) is a potent protein synthesis inhibitor, a puromycin acetylene analog.</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>DRB18 inhibits GLUT proteins, altering glucose metabolism and inducing cancer cell death by G1/S arrest and oxidative stress.</p>

<p>Lometrexol (LY 264618) is an antifolate that inhibits GARFT, blocks purine synthesis, induces apoptosis, and has anticancer properties.</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>Elacytarabine (M7594 0037), a lipid-conjugated derivative of the nucleoside analog cytarabine, is an antineoplastic drug. It has cytotoxicity in solid tumors.</p>

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

<p>BQ-788 is an ETB receptor antagonist with potential hypertensive activity that inhibits exogenous ET-1-induced elevation of coronary perfusion pressure.</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>DRF-1042 is a camptothecin analog with anticancer and insecticidal activity and is used to study solid tumors such as prostate and colon cancer.</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>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>BAY-3827 is an AMPK inhibitor with antiproliferative activity and antitumor activity. BAY-3827 inhibits the phosphorylation of acetyl CoA carboxylase 1.</p>

<p>GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.</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>NRX-103094 boosts β-catenin binding to SCFβ-TrCP ligase with EC50 62 nM and Kd 0.6 nM.</p>

<p>HRO761 is a potent Werne r syndrome RecQ DNA deconjugase (WRN) inhibitor that can be used to study cancers such as colon and stomach cancer.</p>

<p>FABPs ligand 6 (MF6) is an inhibitor of FABP5 and FABP7.</p>

<p>INCB054329 is a BET inhibitor targeting BRD2/3/4 and BRDT with IC50s ranging from 1-119 nM.</p>

<p>NRX-103095 increases β-catenin binding to SCFβ-TrCP E3 ligase; EC50 is 163 nM for pSer33/Ser37 affinity boost.</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>TPX-0131: potent, selective, CNS-ready, oral ALK inhibitor (WT IC50: 1.4nM, G1202R/L1196M IC50: 0.3nM) with robust antitumor effects.</p>

<p>NB-360: potent, brain-penetrant BACE1/2 inhibitor; IC50s: 5-6 nM; high selectivity vs pepsin, cathepsin E/D.</p>

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

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

<p>AZ12601011 is a TGFBR1 kinase inhibitor that inhibits the growth of breast tumors.</p>

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

<p>MAO-B-IN-17 is a selective and potent monoamine oxidase B (MAO-B) inhibitor (IC50: 5.08 μM) for the study of central nervous system disorders like Parkinson's.</p>

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

<p>Iclepertin (BI-425809) is a GlyT1 inhibitor.Iclepertin is used for the treatment of Alzheimer;s disease and other CNS disorders.</p>

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

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

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

<p>VX-984 (M9831) is an oral DNA-PK inhibitor, crossing the blood-brain barrier, targeting GBM and NSC-LC.</p>

<p>BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614</p>

<p>Simmitecan hydrochloride is a camptothecin derivative, a topoisomerase I inhibitor with anticancer activity, which can be used to study is solid tumors.</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>AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor (IC50: 0.42 μM).</p>

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

<p>Glycosyltransferase-IN-1 is a glycosyltransferase inhibitor with bacteriostatic activity, inhibiting MSSA, MRSA, Bacillus subtilis, and Enterobacteriaceae.</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>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>Vofopitant dihydrochloride (GR 205171A) is a tachykinin NK1 receptor antagonist and a potential compound for the treatment of pathologic vomiting.</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>Suzetrigine (VX-548) is an oral NaV1.8 inhibitor with analgesic properties for acute pain research.</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>CP-642931 (Sorbitol dehydrogenase-IN-1) is a sorbitol dehydrogenase inhibitor used in the study of diabetes mellitus and cardiovascular disease.</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>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>ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.</p>

<p>Cort108297: selective GR modulator/antagonist, high GR affinity (Ki: 0.45nM), no other steroid receptor affinity.</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>CP-4126, a lipophilic pro-drug of Gemcitabine, converts to active form by esterases, allowing oral administration with dose-dependent effects.</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>PD151746: calpain inhibitor, Ki μ-calpain=0.26μM, Ki m-calpain=5.33μM; reduces oxLDL cytotoxicity.</p>

<p>LY3143921 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor with broad in vitro anticancer activity [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>SR 11302 is an inhibitor of activator protein-1 (AP-1).</p>

<p>XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.</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>Rolapitant HCl is a potent NK1 antagonist, non-CYP3A4 interactive, with anti-emetic effects and a Ki of 0.66 nM.</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>Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral</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>10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata and possesses high anti-cancer properties.</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>TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4.</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>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>Sebetralstat (KVD900) is an inhibitor of plasma kallikrein and can be used in studies about metabolic diseases.</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>Clorophene (Clorofene) is an antimicrobial agent and can be used in personal care products.</p>

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

<p>N-Octylmaleimide is an alkylmaleimide, which can inhibit rat liver glucose 6-phosphatase.</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>Metrizoic acid is an ionic contrast medium. Metrizoic acid displays high osmolality and has a risk of inducing allergic reactions.</p>

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

<p>(S)-Rasagiline is rasagiline S-isomer, and is an agent of anti-Parkinson.</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>sodium 4-pentynoate is a alkynylacetate analogue.</p>

<p>Cysteinylglycine TFA is an endogenous metabolite. It is used in disease diagnosis.</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>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>Loviride, a reverse transcriptase inhibitor with IC50 of 0.3 μM, blocks HIV-1/2 and SIV in MT-4 cells.</p>

<p>3-Hydroxyhippuric acid is an acyl glycine, which are normally minor metabolites of fatty acids.</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>(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>3-Methylcrotonylglycine is an acyl glycine, a normal amino acid metabolite found in urine.</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>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>

<p>4-Ethoxycoumarin has antimicrobial activity.</p>

<p>EGFR-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.</p>

<p>2'-Hydroxy-4'-methylacetophenone, a phenolic compound isolated from Angelicae koreana roots possesses acaricidal property. 2'-Hydroxy-4'-methylacetophenone has acaricidal activity, it could be used in the preparation of 4'-methyl-2'-[(p-tolylsulfonyl) oxy] acetophenone.</p>