Other Inhibitors

<p>MK-7445 is a conformationally constrained inhibitor of non-nucleoside reverse transcriptase.</p>

<p>Homopteroic Acid, a precursor to Homofolic Acid, inhibits L1210 mouse leukemia growth by targeting folate uptake.</p>

<p>Fluoropolyoxin L exhibits inhibitory activity against Escherichia coli and Enterococcus faecalis.</p>

<p>Miyakamide A2 is an antibiotic with insecticidal properties. It inhibits the growth of brine shrimp and exhibits weak activity against Xanthomonas species. The IC50 for inhibiting P388 cells is 12.2 μg/mL.</p>

<p>AZD-4121 is an oral cholesterol absorption inhibitor targeting NPC1L1 for the treatment of dyslipidaemia.</p>

<p>Z57346765 is a specific PGK1 inhibitor that inhibits PGK1-dependent cell proliferation by decreasing the metabolic enzyme activity of PGK1 during glycolysis.</p>

<p>Oberadilol is a pyridazinone derivative with vasodilatory and beta-adrenergic blocking activities and type III phosphodiesterase inhibitory action</p>

<p>10-Hydroxyundeca-2,4,6,8-tetraynamide is a polyacetylene antibiotic exhibiting activity against Gram-positive and Gram-negative bacteria, yeasts, fungi, as well as cytotoxic properties.</p>

<p>NCATS-SM4487 is a highly selective inhibitor of GALK1 (IC50: 0.05 μM).</p>

<p>Epelmycin C exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria, as well as antifungal activity against Candida albicans. It also shows activity against leukemia L1210.</p>

<p>Fusarielin A is a natural product found in the genus Fusarium.</p>

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

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

<p>Mollisin is a quinone antibiotic with antifungal properties.</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>

<p>BAY-850 is a selective probe targeting Atad2A's bromine domain, displacing acetylated H4 peptides and detaching ATAD2 from chromatin at 1μm.</p>

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

<p>Henagliflozin (SHR3824): an oral, selective SGLT2 inhibitor, weak on SGLT1.</p>

<p>Aplysin suppresses breast cancer cells and protects liver cells by blocking PI3K/AKT/FOXO3a and preventing oxidative damage.</p>

<p>Difeterol is a biochemical.</p>

<p>ENPP1-IN-12 is a potent, oral ENPP1 inhibitor with a Ki of 41 nM and anti-tumor properties.</p>

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

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

<p>FTI-2153 TFA inhibits farnesyltransferase with high selectivity (IC50: 1.4 nM), over 3000x more than Rap1A processing.</p>

<p>GSK3527497: potent TRPV4 inhibitor, IC50=12 nM, targets heart/respiratory issues, for oral/IV use, low-dose effective.</p>

<p>Glutaminyl cyclase inhibitor IsoQC-IN-1: IC50=12 nM for QC, 73 nM for isoQC; blocks CD47/SIRPα; boosts THP-1, U937 macrophage phagocytosis.</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>Compound S-13: Potent hCA II inhibitor, Kis 4.4, 9.2, 480.2, 14.7 nM for hCA II, I, IV, IX. Used in glaucoma research.</p>

<p>OUN58101, also MDK-8101/BI-D, is an RSV L-protein inhibitor with no formal name, first reported in patent WO 2005042530.</p>

<p>MMP408 acts as an inhibitor of MMP-12.</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>BM635 hydrochloride is an MmpL3 inhibitor with outstanding anti-mycobacterial activity (MIC50: 0.12 μM against M. tuberculosis H37Rv).</p>

<p>Netobimin is an anthelmintic effective against naturally acquired gastrointestinal nematodes in cows.</p>

<p>Dimesna (BNP-778), when used in conjunction with active cancer chemotherapy agents, can reduce the toxicity associated with uremia.</p>

<p>Leptofuranin C, found in the Str. tanashiensis strain, is known to arrest normal cell progression and induce cell death.</p>

<p>MPO-IN-8, an orally active myeloperoxidase (MPO) inhibitor, effectively inhibits the production of hypochlorous acid in neutrophils and the release of extracellular traps (NETosis). In mice exhibiting gouty arthritis, it reduces swelling, decreases peroxidase activity, and lowers IL-1β levels.</p>

<p>Iloprost, a potent prostacyclin analog, binds to human IP &amp; EP1 receptors with high affinity; inhibits platelet aggregation effectively.</p>

<p>GSK699 is a potent, cell penetrant PCAF/GCN5 PROTAC.</p>

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

<p>Furaprevir is an HCV NS3/4A Inhibitor</p>

<p>Allosucrose is a biochemical.</p>

<p>Vanin-1-IN-3 (OMP-7) is a vanin-1 inhibitor with an IC 50 of 0.038 μM [1].</p>

<p>TRβ Agonist 1, a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, demonstrates an EC50 value of 21 nM.</p>

<p>KUSC-5037 inhibits HIF-1 (IC50 = 1.2 μM) and mitochondrial complex V/FoF1ATP synthase.</p>

<p>p38-α MAPK-IN-5: potent p38α inhibitor, IC50s: 0.1 nM (α), 0.2 nM (β), 944 nM (γ), 4100 nM (δ); anti-inflammatory, promising for asthma/COPD research.</p>

<p>ETX0282, oral class A/C β-lactamase inhibitor, developed by Entasis with cefpodoxime for bacterial infections.</p>

<p>Antibiotic MA 144M2, an anthracycline glycoside, targets gram-positive bacteria and tumors, derived from Streptomyces and aclacinomycin A conversion.</p>

<p>Balanol is an ATP-competitive Protein Kinase C and Protein Kinase A inhibitor.</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>SARS-CoV-2-IN-23 (compound GRL-0617) is an inhibitor of SARS-COV-2 papain-like protease (PLpro) (IC 50 = 2.3 μM) [1].</p>

<p>Bulgecin A is an inhibitor of binuclear metallo-beta-lactamases and Lytic transglycosolase.</p>

TAK-024 is an inhibitor of platelet(IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively).

<p>DS01080522: PRKACA inhibitor, IC50: kinase 0.8 nM, CREB 66 nM; potential for cancer research.</p>

<p>Tylophorinidine is an antifungal agent that has shown to inhibit cell growth.</p>

<p>Cephemimycin exhibits mild antibacterial and antifungal activity.</p>

<p>Sannamycin G (Istamycin X0) is an aminoglycoside antibiotic that exhibits only weak antibacterial activity against a limited range of bacteria.</p>

<p>SLC7A11-IN-2 (Compound 1) is an inhibitor of SLC7A11/xCT. It disrupts the oxidative balance in HeLa cells by decreasing intracellular glutathione levels and increasing oxidative stress, thereby inducing cell death with an IC50 of 10.23 μM. Molecular dynamics simulations have demonstrated that SLC7A11-IN-2 exhibits a stronger binding affinity to SLC7A11 compared to Erastin. This compound is useful for research in the field of cervical cancer.</p>

<p>Fosfocytocin can be found in the Pseudomonas fluorescens strain PK-52 and exhibits very weak antibacterial activity.</p>

<p>mPGES1-IN-5 (compound 18) is a multi-substituted pyrimidine compound that acts as a submicromolar inhibitor of PGE2 production. It primarily exerts its anti-inflammatory effects by inhibiting mPGES-1 and demonstrates significant inhibitory activity in vivo against acute inflammation models.</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>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>EBOV-GP-IN-1 (Compound 28) is a potent inhibitor of Ebola entry, acting on the Ebola virus envelope glycoprotein (EBOV-GP) (IC50: 0.05 μM).</p>

<p>17β-HSD1-IN-1 (Compound 1) can be used in the non-small cell lung cancer (NSCLC) research.</p>

<p>FXIa-IN-10 is a potent, orally bioavailable inhibitor of Activator XI (FXIa) (Ki: 0.17 nM).</p>

<p>Ganciclovir monophosphate treats CMV, inhibiting replication in human/animal strains (IC50: 0.01μM).</p>

<p>9(R)-HETE, 50% of racemic mix, activates RXRγ 1.5x at 300 nM; identified by HPLC comparison.</p>

<p>AKR1C3-IN-5 inhibits AKR1C3, key in prostate/breast cancers, with MCF-7 cell IC50 of 9.6 μM.</p>

<p>NPR-C activator 1 is an activator of the natriuretic peptide receptor C (NPR-C), which can be used to study cardiovascular diseases.</p>

<p>DJT06001 is a selective Factor Xa inhibitor, reducing thrombus formation with low risk of bleeding.</p>

<p>Anticancer agent 28 is 50x more potent than Oridonin, IC50 of 0.09 μM against K562; effective in H22 mouse tumors.</p>

<p>Axl-IN-3 is a selective, potent and orally active inhibitor of AXL kinase (IC50: 41.5 nM) and has a low inhibitory effect on other kinases.</p>

<p>Olanzapine/Samidorphan, a tablet blending olanzapine and samidorphan, targets schizophrenia and bipolar I, curbing weight gain.</p>

<p>SSM3 TFA is a potent furin inhibitor, blocking furin-dependent cell surface processing of anthrax protective antigen-83 in vitro..</p>

<p>LA-810 is a nitrous oxide donor.</p>

<p>Nurr1 agonist 1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1 which is an appealing target to treat neurodegenerative diseases.</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>UM1 upregulates utrophin, has EC50 of 0.11 μM, useful in DMD research.</p>

<p>Everafenib: potent BRAF inhibitor, crosses blood-brain barrier, hinders MAPK, effective on V600EBRAF cells, outperforms other drugs in trials.</p>

<p>G12Si-1 selectively binds and inhibits K-Ras(G12S) to block oncogenic signaling and nucleotide exchange.</p>

<p>MRS4738 is a potent antagonist with high affinity for the P2Y14R receptor. It demonstrates in vivo anti-hyperallodynic and antiasthmatic activity [1].</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>SCP1-IN-2: potent, selective SCP1 inhibitor; induces REST degradation, hinders its activity, may study REST-driven glioblastoma growth.</p>

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

<p>ZK-Thiazolidinone (TAL), ATP-competitive PLK1 inhibitor, disrupts cell division processes in vitro and in vivo, targeting human/mouse tumors.</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>GLS1 Inhibitor-5 (24y): Selective, oral glutaminase 1 inhibitor; IC50 68 nM; induces apoptosis; anti-tumor.</p>

<p>NTPDase-IN-1 selectively inhibits NTPDases 1, 2, 8 with IC50 of 0.05, 0.23, 0.54 μM. Non-competitive, K m 21 μM, used in cancer, immune, infection research.</p>

<p>GSK1820795A: Telmisartan analog, selective hGPR132a antagonist, blocks yeast activation by N-acylamides, angiotensin II antagonist, partial PPARγ agonist.</p>

<p>PCTR1, derived from DHA, hastens inflammation resolution and boosts macrophage function, reducing PGE2, PGD2, and TXB2 in mice.</p>

<p>ADP-2341 is a soluble analog of FiVe1.</p>

<p>Pim-1 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase, demonstrating an inhibitory concentration (IC50) of 35.13 nM [1].</p>

<p>Detajmium is an anti-arrhythmia compound. It is an Na(+)-channel-blocking drug with an extremely long recovery from use-dependent sodium channel block.</p>

<p>(25S)-delta7-Dafachronic acid, an orphan nuclear receptor DAF-12 ligand, inhibits the dauer-promoting activity of DAF-12.</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>Ici D1542: potent TXS inhibitor &amp; TXA2 receptor antagonist, effective thromboxane blocker in vitro.</p>

<p>BRD-9526 is a potent and selective inhibitor of Sonic Hedgehog (Shh).</p>

<p>L 767679 is an antagonist of the fibrinogen receptors.</p>

<p>SSR-182289A (Free) is a thrombin inhibitor.</p>

<p>Dinordrin is an implantation inhibitor and hormone.</p>

<p>Retelliptine, a DNA topoisomerase II inhibitor, is used potentially for the treatment of cancer.</p>

<p>L 739749 is a CAAX peptidomimetic. It is also an inhibitor of farnesyl-protein transferase.</p>

<p>Naltalimide: µ-opioid receptor partial agonist, improves bladder storage by affecting spinal cord reflex.</p>

<p>Pamiparib (BGB-290) is a selective PARP inhibitor that blocks DNA repair and promotes apoptosis.</p>

<p>Ambelline has antitumor activity.</p>

<p>DI-404: Potent DCN1-UBC12 inhibitor, selectivity blocks cullin 3 neddylation, Kd=6.9 nM.</p>

<p>GSK2578999A is a betulin derivative with antitumor activity.</p>