PSB-1584 | GPR84 Agonist
Potent synthetic exogenous agonist at GPR84 which is selective against other free fatty acid receptors and is metabolically stable when incubated with human liver microsomes.
BTB-1 | Mitotic kinesin Kif18A inhibitor
Selective, ATP-competitive and reversible inhibitor of mitotic kinesin Kif18A. Suppresses the replication of influenza A virus,
Chromomycin A3 | DNA Stain
DNA-binding agent specific for GC-rich sequences which may be used as a DNA stain. Inhibits neuronal apoptosis induced by oxidative stress and DNA damage.
Cytochalasin B | Actin filament disrupting agent
Cell permeable fungal toxin which binds to the barbed end of actin, inhibiting its polymerization. Inhibits cell division, migration and glucose transport.
Oleamide | Endogenous sleep inducing ligand
Displays agonist activity at cannabinoid CB1 receptors. Activates PPARγ. Displays neuroprotective effects and attenuates sepsis-induced intestinal injury.
WP631 | Inhibits SP-1 activated transcription
Potent inhibitor of Sp1-activated transcription. Induces caspase-dependent apoptosis in human ovarian cancer cells.
Tomentosin | Inhibitor of NFkB activation
It suppresses the production of inflammatory mediators by inhibiting NFκB activation. Induces Apoptosis in some cancer cell lines.
Dodecyl-TPP | Mitochondrial-targeted cancer stem cell inhibitor
Inhibits mitochondrial function inhibiting oxidative phosphorylation and shifting cell metabolism to glycolysis. Potently eradicates cancer stem cells selectively over normal cells.
4-MUG | beta-Glactosidase fluorogenic substrate
Versatile fluorogenic substrate for β-galactosidase1 for use in cell extracts or purified enzyme preparations.
AE 51310 | OPN4/Melanopsin antagonist
Potent antagonist of the GPCR OPN4/melanopsin. OPN4 regulates circadian rhythms, pupil functions, melatonin expression, cognition, and sleep.
BO-264 | TACC3 inhibitor
Potent inhibitor of transforming acidic coiled-coil 3 (TACC3), an important protein involved in microtubule stability and centrosome integrity.
Ipatasertib | Pan-AKT inhibitor
Selective and potent pan-Akt inhibitor. It displayed efficacy in xenograft models of prostate, breast, ovarian, colorectal, non-small cell lung, glioblastoma, and melanoma cancers.
SX-682 | CXCR1/2 inhibitor
Novel CXCR1/2 inhibitor. It displayed robust synergistic activity with immune checkpoint blockade against castration resistant prostate cancer.
Brigatinib | pan-ALK inhibitor
Potent and selective pan-ALK inhibitor. Cells with ALK mutation L1196Q2 and the double mutation I1171S + G12693 remain sensitive to brigatinib.
AS-1949490 | SHIP2 inhibitor
Potent and selective inhibitor of the intracellular phosphatase SHIP2. Displays ca. 30-fold selectivity for SHIP2 over SHIP1.
WH-4-023 | Src family inhibitor
Potent and selective Src family kinase inhibitor known to inhibit Lck, Src, SIK1, SIK2 and SIK3.
NQDI-1 | ASK1 inhibitor
Selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1). Promotes survival of induced pluripotent stem cells.
Filgotinib | JAK1 inhibitor
Potent and selective JAK1 inhibitor. Displays potent anti-inflammatory activity in various models.
CPI-613 | KGDH and PDH inhibitor
Lipoic acid analog which potently disrupts mitochondrial metabolism with selectivity for tumor cells in vitro and shows strong antitumor activity in vivo.
Dyclonine HCl | Mitochondrial function enhancer
Topical anesthetic which has been used for oral and throat analgesia. Enhances neuronal mitochondrial function, potentiating respiration and providing protection against insults associated with neurodegenerative disorders.
URMC-099 | Mixed-lineage kinase inhibitor
Potent, brain penetrant mixed-lineage kinase 3 inhibitor (MLK3). It also potently inhibits FLT3, LRRK2, and ABL1.
PFI-3 | Family VIII bromodomain inhibitor
Selective inhibitor of family VIII bromodomains PB1(5), SMARCA2, and SMARCA4. Shows complete selectivity over all non-family VIII bromodomains.
PB28 dihydrochloride | High affinity sigma 2 ligand / Anti-SARS-CoV2
Very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist. Selective for σ2 over σ1. PB28 inhibited cell growth in MCF7 and MCF7 ADR breast cancer cells and displayed strong synergism with doxorubicin
Liproxstatin-1 | Ferroptosis inhibitor
Inhibitor of ferroptosis. Liproxstatin-1’s mechanism of activity has been attributed to its activity as a radical-trapping antioxidant.
GSK2982772 | RIPK1 inhibitor
Highly selective inhibitor of Receptor-interacting Protein 1 kinase.
Fludarabine | DNA synthesis inhibitor
Synthetic adenosine analog that inhibits DNA biosynthesis and is a clinically useful antineoplastic agent.
FITC-Tyramide | Signal amplification reagent for immunoassays
Reagent for use in catalyzed reporter deposition (CARD) signal amplification1 protocols in a variety of immunoassays in which horseradish peroxidase catalyzes local deposition of FITC tyramide.
Xanomeline tartrate | Selective M1 muscarinic agonist
Functionally-selective M1 muscarinic receptor agonist. Displays positive cognitive and behavioral effects in schizophrenia and Alzheimer’s disease. Suppresses proinflammatory cytokine responses and improves survival in sepsis.
Emetine hydrochloride | Protein synthesis inhibitor
A useful agent for inhibiting protein synthesis in eukaryotic cells by virtue of its inhibition of the ribosome 40S subunit. Inhibits Zika and Ebola virus in vitro and in vivo, also inhibits SARS-CoV-2 replication in cells
Boceprevir | Antiviral, SARS-CoV2 Mpro inhibitor
Directly inhibits Hepatitis C virus (HCV) NS3 protease. This blocks NS3 autoactivation, and subsequent cleavage and maturation of other viral proteins necessary for replisome assembly.
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).