Altri inibitori

<p>NA 382 is a staurosporine derivative that inhibits multidrug resistance.</p>

<p>Ici D1542: potent TXS inhibitor &amp; TXA2 receptor antagonist, effective thromboxane blocker in vitro.</p>

<p>Cytochalasin F reversibly inhibits cytokinesis and possesses various biological activities including the inhibition of macrophage endocytosis and exocytosis.</p>

<p>ATM-3507 trihydrochloride is a potent tropomyosin inhibitor (IC50s: 3.83-6.84 μM in human melanoma cell lines).</p>

<p>OM-153 blocks tankyrase 1 (IC50: 13 nM) and 2 (IC50: 2 nM), stifling WNT signaling and COLO 320DM cell growth.</p>

<p>Haliangicin A exhibits antifungal activity against filamentous fungi and also affects oomycetes, though it does not possess antibacterial properties.</p>

<p>Adecypenol is a unique adenosine deaminase inhibitor. It shows effective inhibitory activity against calf intestinal adenosine deaminase.</p>

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

<p>Espinomycin A3 is a 16-membered macrolide antibiotic (antibiotic) that exhibits activity against Gram-positive bacteria.</p>

<p>Oxeclosporin is a hydroxyethyl derivative of serine(8)-cyclosporine; inhibits proliferation and functions of lymphocytes.</p>

<p>2-n-Heptyl-4-quinolinol exhibits activity against Candida albicans, Staphylococcus aureus, Vibrio anguillarum, and Vibrio harveyi.</p>

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

<p>Plumbemycin A is isolated from Streptomyces plumbeus; an L-threonine antagonist.</p>

<p>CL656 is a stimulator of interferon genes (STING) activator.</p>

<p>KF 20274 is an adenosine A1 antagonist; purinergic receptor antagonist.</p>

<p>Lp-PLA2-IN-6: Potent tetracyclic inhibitor of rhLp-PLA2, with pIC50 of 10.0, and potential in neurodegenerative research.</p>

<p>VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent inhibitor of VEGFR-2 (IC50: 0.037 μM). VEGFR-2-IN-12 has anti-tumour effects.</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>Formadicin A exhibits strong activity against various Pseudomonas, Proteus, and Alcaligenes bacteria.</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>ZIKV-IN-4 is a low cytotoxic, acid-stable anti-ZIKV agent with an EC50 value of 3.49 μM. ZIKV-IN-4 exhibited potent inhibition of ZIKV NS5 MTase.</p>

<p>FCE-27262 is a prostaglandin H2/thromboxane A2 receptor antagonist.</p>

<p>Alphavirus-IN-1 blocks VEEV (EC50: 0.24 μM) &amp; EEEV (EC50: 0.16 μM), non-toxic, stable in mice plasma.</p>

<p>SPR7 is a potent and selective rhodesain inhibitor (Ki: 0.51 nM). SPR7 exhibited antiparasitic effects against T. b. brucei (EC50: 1.65 μM).</p>

<p>Odiparcil is an orally active beta-d-thioxyloside analog.</p>

<p>Benadrostin is a Poly(ADP-ribose) synthetase inhibitor with an IC50 of 35μM.</p>

<p>PD-1/PD-L1-IN-16 is a potent inhibitor of PD-1/PD-L1 (IC50: 53.2 nM) and has shown research potential for tumour immunotherapy.</p>

<p>D6808: selective c-Met inhibitor, IC50=2.9 nM, induces apoptosis and cell cycle arrest, for NSCLC/gastric cancer research.</p>

<p>5-Deoxygentamicin C1 exhibits activity against both gram-positive and gram-negative bacteria.</p>

<p>Topoisomerase I inhibitor 8, a hexacyclic analogue of camptothecin, is also a potent inhibitor of topoisomerase I and is toxic to tumour cells.</p>

<p>MK-7128 is a CB1 receptor inverse agonist.</p>

<p>Oiligodendrocyte differentiation promoter 1 is a promoter of oiligodendrocyte differentiation .</p>

<p>Unoprostone is a prostaglandin F2α analogs (PGAs), and reduces intraocular pressure and is used topically for glaucoma or ocular hypertension.</p>

<p>1-Deamino-1-hydroxygentamicin C2 (AntibioticSU-1) is an aminoglycoside antibiotic effective against both Gram-positive and Gram-negative bacteria.</p>

<p>Carpetimycin C exhibits strong activity against both Gram-positive and Gram-negative bacteria, including those that produce β-lactamase. It also has a powerful inhibitory effect on β-lactamase .</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>SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor.</p>

<p>Dehydroindapamide, an indole form of Indapamide, is utilized to quantify the turnover rate of Indapamide in CYP3A4, which is approximately 10 times higher than that of Indoline, with slightly enhanced affinity for CYP3A4.</p>

<p>9-O-Demethyltrigonostemone is a natural IDO1 inhibitor, cytotoxic and antiplasmodial agent from the Roots of Strophioblachia fimbricalyx.</p>

<p>PD-149163: brain-penetrating, selective NTR1 agonist; shows pro-cognitive, anti-psychotic, anxiolytic effects.</p>

<p>nNOS-IN-25 is an effective, selective, and cell-permeable inhibitor of neuronal nitric oxide synthase.</p>

AT-IAP is an effective dual antagonist of XIAP and cIAP1.

<p>Rhodomycin B exhibits activity against Gram-positive bacteria, while its effects on Gram-negative bacteria and fungi are relatively weak.</p>

<p>ML-SI1, a racemic mixture of diastereoisomers, is a TRPML inhibitor and acts on TRPML1 (IC50: 15 μM).</p>

<p>Griseolutein A exhibits activity against both Gram-positive and Gram-negative bacteria.</p>

<p>Pelagiomicin C exhibits activity against both Gram-positive and Gram-negative bacteria.</p>

<p>Schidigera-genin B is a steroidal saponin that can be isolated from Yucca glauca. It exhibits mild antifungal activity.</p>

<p>FTI-2628 is a novel inhibitor of protein farnesyltransferase (FT), inhibiting the growth of P. falciparum in red blood cells and suppressing parasitemia.</p>

<p>Isobetanin is a betacyanin that has been shown to enhance vitexin-2-O-xyloside mediated inhibition of proliferation of T24 bladder cancer cells.</p>

<p>Methylenomycin B is a cyclopentanone-derived antibiotic effective against both Gram-negative and Gram-positive bacteria.</p>

<p>Saframycin Mx2 exhibits activity against both Gram-positive and Gram-negative bacteria.</p>

<p>Chitinovorin C is a β-lactam class antibiotic (antibiotic) that exhibits weak inhibitory activity against Gram-negative bacteria.</p>

<p>Mycelianamide is an antibiotic effective against Gram-positive bacteria.</p>

<p>4-Hydroxyphlebiarubrone is a quinone antibiotic. It exhibits weaker resistance against Gram-negative bacteria and possesses cytotoxic properties.</p>

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

<p>UH 301 is a 5-HT1A receptor antagonist.</p>

<p>TrxR-IN-5 (compound 4f) is an effective inhibitor of thioredoxin reductase (TrxR) with an IC₅₀ of 0.16 μM. anti-proliferative and anti-metastatic.</p>

<p>Heme Oxygenase-2-IN-1 is a selective HO-2 inhibitor with IC50s: 14.9 μM (HO-1), 0.9 μM (HO-2).</p>

<p>Saframycin B exhibits activity against Gram-positive bacteria and has weaker efficacy against mycobacteria.</p>

<p>Gusperimus was synthesized by chemical modification of spergualin and in combination with cyclosporine A to prevent diabetes in susceptible NOD mice.</p>

<p>Panosialin wA inhibits α,β-glucosidase and mannosidase enzymes, but does not exhibit inhibitory activity against the influenza virus. However, it has a mild antibacterial effect.</p>

<p>Dihydrobisdechlorogeodin, produced by the fungus strain [FO-4712] of the genus Acremonium, serves as a herbicide.</p>

<p>MDK-3298 is a reversible covalent inhibitor of Mcl-1, a target of protein-protein interaction (PPI).</p>

<p>SARS-CoV-2-IN-6 is an inhibitor of SARS-CoV-2 3CLpro with the IC 50 value of 73 nM.</p>

<p>ZK168281 is a 1α,25(OH)2D3 analog, VDR antagonist with 0.1 nM Kd, and blocks receptor CoA interaction.</p>

<p>Enpp-1-IN-11 inhibits ENPP1 with a 45 nM Ki, is plasma stable, and has low clearance in human/mouse livers, potentially aiding cancer research.</p>

<p>DC41SMe, a DC1 derivative and CC-1065 analogue, targets cancer with 18-25 pM IC50 against Ramos, Namalwa, HL60/s cells.</p>

<p>AZD-3409 is a more potent prenyl transferase inhibitor than lonafarnib with varied IC(50) in cells, acting on gefitinib-resistant breast cancer.</p>

<p>FTI-2148 blocks RAS-related FT-1 &amp; GGT-1; IC50: 1.4 nM &amp; 1.7 μM.</p>

<p>Eponemycin is an antibiotic with antitumor properties. It exhibits cytotoxicity against cancer cell lines B16-F10, L1210, P388, and HCT-116, with IC50 values of 0.0017, 0.01, 0.031, and 0.0097 µg/mL, respectively. In B16-F10 and mitomycin C, Eponemycin inhibits DNA synthesis, with IC50 values of 0.1 µg/mL and 0.41 µg/mL, respectively.</p>

<p>Guraxetan can be used in the synthesis of the antitumour drug Lutetium (177Lu) zadavotide Guraxetan.</p>

<p>(-)-Adenophorine is a moderate alpha-l-fucosidase inhibitor.</p>

<p>SARS 3CLpro-IN-1: stereospecific SARS 3CL protease inhibitor, octahydroisochromene class, IC50 = 95 μM.</p>

<p>Halomicin B is an ansamycin-type antibiotic effective against both Gram-positive and Gram-negative bacteria.</p>

<p>Phencomycin exhibits mild activity against Gram-positive bacteria and inhibits physiologically important enzymes such as renin, with an IC50 of 440 μg/mL.</p>

<p>ND-654 is an acetyl CoA carboxylase inhibitor.</p>

<p>Dechloromycorrhizin A is an antibiotic with weak activity against Gram-positive bacteria, yeasts, and molds, but it exhibits strong nematocidal activity.</p>

<p>Nafarelin: a GnRH agonist used to treat endometriosis, precocious puberty, and control IVF. Delivered as a nasal spray. Marketed as Synarel by Pfizer.</p>

<p>Naphthoquinomycin A is an antibiotic that exhibits activity against Gram-positive bacteria and fungi, and also inhibits the synthesis of fatty acids in Escherichia coli.</p>

<p>Cofpropamine, a caffeine derivative that inhibits polyadenylation, enhances the suppressive effects of Cyclophosphamide in animal models of rat adjuvant arthritis and mouse collagen-induced arthritis.</p>

<p>(6S)-CP-470711 (Compound 8) acts as an inhibitor of sorbitol dehydrogenase (SDH) in both humans and rats, exhibiting inhibitory concentrations (IC50) of 19 nM and 27 nM, respectively. Additionally, (6S)-CP-470711 has been shown to ameliorate diabetes in rats induced by Streptozotocin.</p>

<p>S24-14 serves as an effective anti-osteoporosis agent by inhibiting osteoclastogenesis, promoting osteoblast differentiation, and reducing bone resorption.</p>

<p>P2X receptor-1 is a potential inhibitor of P2X receptor for the treatment of pain and inflammation.</p>

<p>Pacidamycin 5 exhibits inhibitory effects on Pseudomonas aeruginosa. It is also effective against certain strains of Staphylococcus aureus and Escherichia coli.</p>

<p>WS-898 boosts paclitaxel efficacy in resistant cells by inhibiting ABCB1; IC50: SW620/Ad300 - 5.0 nM, KB-C2 - 3.67 nM, HEK293/ABCB1 - 3.68 nM.</p>

<p>RXR antagonist 2 is a potent antagonist of RXR (Ki: 0.391 μM, Kd: 0.281 μM). RXR antagonist 2 has shown research potential for RXR-related diseases.</p>

<p>NUCC-555 is a first-in-class antagonist of activin. It opens a completely new approach to inhibiting the activity of TGF-beta receptor superfamily members.</p>

<p>9(S),10(S),13(S)-TriHOME is an oxylipin derived from linoleic acid. It has been detected in beer and in bronchoalveolar lavage fluid (BALF) from female smokers.</p>

<p>CGS 22652 has thromboxane receptor antagonism combined with thromboxane synthase inhibition.</p>

<p>Fonsartan: Angiotensin receptor blocker, halts angiotensin II effects on rat vascular cells.</p>

<p>Hynapene C exhibits an inhibitory minimum inhibitory concentration (MIC) of 34.7 μM against Eimeria acervulina.</p>

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

<p>PTP1B-IN-18 is an orally active, fully mixed protein tyrosine phosphatase 1B (PTP1B) inhibitor (Ki: 35.2 μM).PTP1B-IN-18 can be used to study type 2 diabetes.</p>

<p>GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 200 nM and 35 nM for hTRα and hTRβ, respectively.</p>

<p>AVE 0991 is a nonpeptide analog of angiotensin-(1-7), a Mas agonist with inhibitory effects on [125I]-Ang-(1-7) and on neuroinflammation in Alzheimer's disease.</p>

<p>Kurasoin A is an inhibitor of the enzyme farnesyltransferase.</p>

BILA 1906 BS is an inhibitor of substrate analog protease.

<p>Thielavin B, from Thielavia terricola, inhibits prostaglandin E2 synthesis and reduces rat oedema.</p>

<p>ZBH-1205, a camptothecin derivative, shows strong antitumor effects via apoptosis, outperforming cpt-11 and sn38 in topoisomerase-1 inhibition.</p>

<p>Antibiotic LL Z1640-2 is an inhibitor against the TAK1 activity.</p>

<p>TY 11345 is a proton pump inhibitor.</p>

<p>eIF4A3-IN-4 is a novel inhibitor of eIF4A (IC50: 8.6 μM).</p>

<p>Gepotidacin (GSK-2140944) is a potent DNA topoisomerase inhibitor, a novel antibacterial efficacious against various anaerobes.</p>

<p>Hydroxyethyl disulfide can counteract the inhibitory effects of showdomycin on methotrexate-resistant thymidylate synthase and is protected from deactivation by its substrate, deoxyuridine monophosphate, thus preserving the antibiotic's activity.</p>

<p>ZK824859 hydrochloride: oral, selective uPA inhibitor, IC50s: 79 nM (uPA), 1580 nM (tPA), 1330 nM (plasmin).</p>

<p>11-Deoxy-13-deoxodaunorubicin is an anthracycline antibiotic with activity against Gram-positive, Gram-negative bacteria, and tumors.</p>