Remodelin | Acetyltransferase NAT10 inhibitor
Potent and selective inhibitor of N-acetyltransferase 10 (NAT10) which us capable of acetylating microtubules and histones. Improves nuclear architecture, chromatin organization and fitness, normalizing progeric and aging cells.
Guggulsterone-(Z) | FXR antagonist
Natural steroid which lowers cholesterol and acts as an FXR antagonist. Induces differentiation of pluripotent stem cells to dopaminergic neurons.
Omeprazole | Proton pump inhibitor/ Antiviral
H+,K+-ATPase inhibitor, clinically useful antisecretory and antiulcer agent. Displays broad spectrum antiviral activity and enhances the efficacy of remdesivir.
GKT-37831 | NADPH oxidase NOX1/4 inhibitor
GKT137831 inhibits NADPH oxidase BOX1/4 and blocks erastin-stimulated ROS production.
TIC10 | Mitochondrial caseinolytic protease P activator / Anticancer agent
Novel anti-cancer compound that acts via early-stage integrated stress response activation leading to selective cancer cell death
Roxadustat | Proyl hydroxylase domain inhibitor / HIF stabilizer
Pan-prolyl hydroxylase domain (PHD) inhibitor that stabilizes hypoxia-inducible factor (HIF) leading to erythropoiesis.
Tiagabine hydrochloride | GABA transporter 1 (GAT1) inhibitor
Clinically useful anticonvulsant that inhibits both neuronal and glial GABA re-uptake
Favipiravir | Inhibitor of viral RNA-dependent RNA polymerase
Inhibitor of viral RNA-dependent RNA polymerase with activity against influenza viruses A,B and C as wells as a wide range of other viruses.
Oseltamivir Phosphate | Neuraminidase inhibitor / Antiviral
Potent viral neuraminidase inhibitor and clinically useful treatment for influenzas A and B.
Ritonavir | HIV1/2 protease inhibitor
Clinically useful HIV-1/HIV-2 protease inhibitor. Potent inhibitor of cytochrome P450 3A4.
GRL-0496 | SARS-CoV 3CLpro inhibitor
Potent inhibitor of severe acute respiratory syndrome-coronavirus chymotrypsin-like protease.
GRL-0617 | Potent SARS-CoV PLpro inhibitor
Potent noncovalent inhibitor of severe acute respiratory syndrome-coronavirus papain-like protease. Inactive against human DUB-like proteases.
Nelfinavir mesylate | HIV protease inhibitor / Anticancer activity
Clinically useful anti-HIV acting via inhibition of HIV-1 proteases. Also displays efficacy in cancer, malaria, tuberculosis and SARS.
Prochlorperazine maleate | Endocytosis inhibtior
Inhibits dynamin and clathrin-mediated endocytosis. Increases tumor cell antigen presentation.
Tazemetostat | EZH2 inhibitor
Potent and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2
Ponatinib | Bcr-Abl multikinase inhibitor
Highly potent pan-Bcr-Abl and multikinase inhibitor, suppressing the activity of native Bcr-Abl as well as the mutants T315I, Q252H, Y253F, M351T and H396P. Protects against influenza A virus-induced death by suppressing cytokine storm in mouse models.
Santacruzamate A | Ultrapotent HDAC2 inhibitor
Highly potent and selective inhibitor of HDAC2 isolated from the Panamanian marine cyanobacterium cf. Symploca.
Brequinar sodium | Dihydroorotate dehydrogenase inhibitor, antiviral
Inhibitor of dihydroorotate dehydrogenase with broad antiviral activity against flaviviruses, positive-strand RNA alphaviruses, negative-strand RNA rhabdoviruses, influenza A and B viruses and HIV.
Roxatidine | Histamine H2 antagonist, antiulcer, anti-inflammatory
Novel histamine H2 receptor antagonist that suppresses inflammatory response via inhibition of NF&kappa>B and p38 MAPK activation in macrophages.
N4-Hydroxycytidine | Novel antiviral
N4-Hydroxycytidine is the active molecule in the antiviral pro-drug clinical candidate EIDD-2801 with action against a broad range of viruses including coronaviruses
Camostat mesylate | Serine protease inhibitor, antiviral, anti-inflammatory activity
Reduces infection of Calu-3 lung cells by SARS-CoV-2 (responsible for COVID-19) via inhibition of the serine protease TMPRSS2 required for viral spike protein priming.
Scriptaid | HDAC inhibitor
Inhibits HDACs 1,3 and 8. Induces cell cycle arrest and epigenetic changes in colon cancer cells.
Dihydroresveratrol | Resveratrol metabolite
Glucuronide conjugates of dihydroresveratrol are found in human urine after oral intake of resveratrol dietary supplements.
DY131 | Estrogen-related receptor ERRβ and ERRγ agonist
Selective agonist at estrogen-related receptors ERRβ and ERRγ with minimal activity at ERRα, ERα and ERβ. Displays antiproliferative activity in prostate cancer cells.
PK150 | Sorafenib analog with unique antibacterial properties
Displays significant antibacterial activity against S. aureus NSTC8325, vancomycin-resistant enterococci and M. tuberculosus. Inactive against Gram-negative bacteria
Leelamine | Intracellular cholesterol inhibitor
Induces cholesterol accumulation in lysosomal/endosomal cell compartments via inhibition of autophagic flux
NU7441 | DNA-PK inhibitor
Potent and selective ATP-competitive inhibitor of DNA-dependent protein kinase. Increases radio/chemosensitivity of various cancer cell lines.
Crenolanib | PDGF and FLT3 inhibitor
Potent inhibitor of PDGFR and FLT3 that binds only to the active kinase configuration.
AZ3146 | Mps 1kinase inhibitor
Potent and selective inhibitor of monopolar spindle 1 that decreases hepatocellular carcinoma growth in vitro.
AZD7762 | Checkpoint Kinase 1/2 inhibitor
Potent and selective inhibitor of checkpoint kinases 1 and 2. It abrogates DNA damage-induced S and G2 checkpoints and enhances the efficacy of DNA damaging agents such as gemcitabine and irinotecan.
SNS-314 mesylate | Aurora kinase inhibitor
Potent and selective Aurora kinase inhibitor. Able to inhibit proliferation in a wide panel of human cancer cell lines.
Elafibranor | PPARalpha/delta agonist
Able to decrease plasma triglycerides levels, increase HDL cholesterol levels in human studies, and improve hepatic and peripheral insulin sensitivity.
Levetiracetam | Anticonvulsant
Clinically useful non classical anticonvulsant believed to act through binding to SV2A. No effect on voltage-dependent Na+ channels, GABAergic transmission, or affinity for either GABAergic or glutaminer rgic eceptor.
Tigecycline | Antibiotic
Clinically useful antibiotic that has also been shown to be selectively toxic to human acute myeloid leukemia cells over normal hematopoietic cells.
Volasertib | Potent and selective inhibitor of Polo-like kinase 1
Potent and selective inhibitor of Polo-like kinase 1 that has shown efficacy in multiple solid xenograft tumor models and in clinical studies of patients with acute myeloid leukemia.
Fruquintinib | Potent and selective inhibitor of VEGFR kinase
Potently and selectively inhibits VEGF/VEGFR signaling and cell proliferation in HUVECs and HLECs and prevents angiogenesis in vitro.
AZ20 | ATR kinase inhibitor
Combination therapy with AZ20 and gemcitabine resulted in synergistic inhibition of tumor cell growth and cell death initiation in pancreatic cancer cell lines.
AZD1152-HQPA | Aurora B kinase inhibitor
Highly selective inhibitor of Aurora kinase B that inhibits the growth of tumors in multiple cancer models.
Lomeguatrib | MGMT inhibitor
Potent inhibitor of O6-Methylguanine-DNA Methyltransferase (MGMT), an important DNA repair protein.
Methoprene Acid | Selective RXR agonist
Binds directly and selectively to the retinoid X receptor (RXR) acting as a transcriptional activator with no activity at RAR. Negatively regulates thrombosis and hemostasis.
ML-335 | Trek-1,2 activator
Novel, selective TREK-1,2 activator with EC50s of 14.3 and 5.2 µM
NOTUMib-1 | NOTUM inhibitor, restores Wnt signaling
Inhibits the carboxylesterase activity of NOTUM, IC50=0.085 µM, and restores Wnt signaling.
MitoBloCK-12 | Mitochondrial import inhibitor
Blocks translocation of a mutant form of alanine: glyoxylate aminotransferase (AGT) to the mitochondria and restores AGT trafficking to peroxisomes.
N-Eicosanoyl serotonin | Neuroprotective
Inhibits the PP2A methylesterase maintaining PP2A in a highly active state leading to hyperphosphorylat αed -synuclein.
DO264 | ABHD12 inhibitor
Potent, reversible competitive inhibitor of ABHD12 (α/β-hydrolase domain-containing 12) which shows negligible interaction with other serine hydrolases.
Rucaparib phosphate | PARP1 inhibitor
Potent PARP1 inhibitor. Cytotoxic to human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2.
Pomalidomide | Cereblon ubiquitination inhibitor
Inhibits the E3 ubiquitin ligase cereblon (CRBN). Displays antiangiogenic and immunomodulatory activity in vivo potently inhibiting the production of TNF alpha and IL-2.
Imiquimod | TLR7 agonist
Toll-like receptor 7/8 agonist with anti-viral and anti-tumor properties. Enhances innate immune system leading to Th1-mediated antitumor immune response.
Norfluoxetine HCl | Fluoxetine Metabolite
Induces long QT syndrome via slow delayed rectifier potassium current block. Time dependent inhibitor of CYP2C19 and CYP3A4.
Acalabrutinib | Highly selective BTK inhibitor
Hghly selective, potent (IC50 = 3nM), and irreversible inhibitor of Bruton’s tyrosine kinase (BTK). Significantly inhibits BCR signaling, inhibits tumor proliferation, and reduces tumor burden.
Ibrutinib | BTK inhibitor
Very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR).