Potent and selective p53-MDM2 binding inhibitor

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel potent, orally bioavailable CXCR2 receptor antagonist

Novel potent, orally bioavailable CXCR2 receptor antagonist

Novel phosphodiesterase 4D (PDE4D) inhibitor

Novel Inhibitor of the Cysteine Protease Cathepsin K

Novel potent and selective antagonist of somatostatin receptor subtype SST(3)

Novel BCR-ABL Kinase Inhibitor

Novel dual inhibitor of TORC1 and TORC2

Novel potent Jak2 type 1 inhibitor

Novel potent and selective p53-HDM2 inhibitor

Potent, orally active dipeptidyl peptidase (DPP)-IV inhibitor

Novel peptide deformylase (PDF) inhibitor; Antibacterial

Novel Syk inhibitor

Novel nonpeptide bradykinin B1 receptor antagonist

The first non-peptide somatostatin sst(1) receptor antagonist

Novel focal adhesion kinase (FAK) inhibitor, potently blocking kinase activity of FAK along with Aurora A, activated Cdc42-associated kinase 1 (ACK1), Met, insulin receptor (IR), TrkA, and IGF-1R

Specific inhibitor of the 25-hydroxyvitamin D(3)-24-hydroxylase (24-hydroxylase)

Novel potent PKCθ inhibitor

Novel selective bromodomain and extra-terminal domain (BET) protein family inhibitor (BETi ), inducing an ‘activated’ keratinocyte transcriptional profile with reversal of chronic wound biomarkers in human skin ex vivo

Novel Potent and Selective inhibitor of YEATS proteins

Negative control for NVS-PAK1-1 (8778)

Potent, orally active, small-molecule enhancer of SMN2 splicing, binding to and stabilizing the U1 snRNP:5′ss RNA complex

Exceptional oxygen transporter, increasing brain tissue oxygen tension (PbtO2) when administered soon after traumatic brain injury (TBI)

Highly potent, selective, reversible, and orally active monoamine oxidase B inhibitor

Novel potent Hsp90 inhibitor, inducing tumor regression in a genetically engineered mouse model of glioblastoma multiforme

Selective nNOS inhibitor and a5-HT1B/1D receptor agonist

Anti-microbial agent against Mycobacterium smegmatis and Mycobacterium bovis BCG, binding to DNA and inducing a unique morphological change to mycobacterial bacilli leading the bacterial cell death

Cancer-testis antigen (CTA) with re-expression in numerous cancer types, eliciting spontaneous humoral and cellular immune responses, restricting expression pattern, being a good candidate target for cancer immunotherapy

Novel water-soluble nystatin derivative, being fully water-soluble (up to 1 g/mL) with the same potency of Nystatin but with 13.5 times lower toxicity

Potent CB1 receptor antagonist

Novel inhibitor of advanced stages of breast cancer, targeting multiple cannabinoid anti-tumour pathways

Novel GPR18 antagonist, blocking the effects of Abn-CBD and NAGly.

Poly(ADP-Ribose) Glycohydrolase (PARG) inhibitor

Novel Selective and Orally Bioavailable Inhibitor of Human Acidic Mammalian Chitinase (hAMCase)

Potent agonist of the human 5-HT2A and 5-HT2C receptors

Natural potent antineoplastic agent with promising in vivo activity in glioblastoma and breast cancer through the activation of oxidative stress

Inhibitor of mitochondrial Lon protease and activator of DNA damage checkpoints

Specific inhibitor of vaccinia-related kinase 1 (VRK1)-mediated phosphorylation of barrier-to-autointegration factor (BAF)

Novel potent antileishmanial and antitrypanosomal agent, offering a more optimal balance of increased solubility, suitable metabolic stability, excellent oral bioavailability (100%), and strong in vivo efficacy in a visceral leishmaniasis mouse model (97%

Blue fluorescent labeling reagent

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

Potent non-prostanoid inhibitor of platelet aggregation, acting via the prostacyclin receptor

Agonist of sst2, sst3 and sst5 somatostatin receptors

Novel highly potent and selective M3 muscarinic acetylcholine receptor antagonist and weak inverse agonist

Novel highly potent and selective M3 muscarinic acetylcholine receptor antagonist and weak inverse agonist

Novel highly potent and selective M3 muscarinic acetylcholine receptor antagonist

Novel highly potent and selective M3 muscarinic acetylcholine receptor antagonist

Cell-permeable, fluorescent Ca2+ indicator

Novel potent O-GlcNAcase (OGA) inhibitor (IC 50 : 46 nM), increasing the level of O-GlcNAcylated protein in cells and displaying suitable pharmacokinetic properties and brain permeability

Novel HSF1 inhibitor for target-based cancer therapy

Novel luciferin analog, enabling both sensitive and highly resolved imaging in vivo

Novel Bax activator, having greatest effect enhancing the pro-apoptotic activity of Bax with EC50 values of ∼0.1 μM and ∼0.9 μM, respectively, inducing cell death by a Bax/Bak-dependent mechanism

Novel orally bioavailable potent JAK-1 inhibitor

Inhibitor of type 1 and type 2A protein phosphatases; Tumor promotor

Inhibitor of type 1 and type 2A protein phosphatases; Tumor promotor

Inhibitor of type 1 and type 2A protein phosphatases; Tumor promotor

Dopamine antagonist as an atypical antipsychotic

Combination of the atypical antipsychotic olanzapine and opioid receptor antagonist samidorphan for treatment of adults with schizophrenia or bipolar I disorder

Natural inhibitor of the phosphorylation of protein kinase C ζ (PKCζ) at Thr410 site, reducing the activation of NF-κB using gain- and loss-of-function approaches in PE-treated cardiomyocytes, ameliorating pressure overload-induced cardiac hypertrophy

Potent antioxidant and neuroprotectant for treatment of Parkinson's disease, reducing reactive oxygen species (ROS) levels, inhibiting extracellular signal-regulated kinase (ERK) 1/2 phosphorylation, reducing rotenone-induced up-regulation of the proapopt

Novel specific agonist of odorant receptor 895 (Olfr895)

Novel Bruton's tyrosine kinase inhibitor, suppressing B cell and monocyte activation and ameliorates arthritis in a mouse model

Phosphodiesterase III inhibitor, augmenting cerebral blood flow by a direct vasodilator effect on cerebral arteries

Novel potent DAGL inhibitor, inhibiting collagen-, but not arachidonic acid-induced aggregation and TxA2 synthesis

Non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I

Potent analogue of oncrasin-1 with antitumor activity mediated by JNK activation and STAT3 inhibition

Novel non-ATP-competitive inhibitor of BCR-ABL, overriding imatinib resistance

Novel enhancer of Schwann cell differentiation for treatment of peripheral nerve disorder

Protease inhibitor

Lipid A analog, inducing Th1-type immune response in tumor eradication and restoring nitric oxide production by peritoneal macrophages

Potent, orally available dual CysLT1 and CysLT2 receptor antagonist

Highly selective agonist of prostaglandin E2 receptor (EP2)

Novel selective EP2 receptor agonist, inducing relaxation of smooth muscle

Novel agonist of the prostaglandin PGE2 receptor EP4

EP(4)-selective antagonist

Novel selective EP3 receptor agonist

Potent, selective, and orally active prostaglandin D2 receptor antagonist

Novel potent inhibitor of protein-protein interactions

Metabolite of Cilostazol

Antioxidant and free radical scavenger, attenuating edema formation, and subsequent tissue damage following cortical contusion

Inhibitor of calmodulin action in calcium regulation

Novel negative allosteric modulator (NAM) of mGlu4, being isomerized with blue-light/dark cycles with fast relaxation

Novel Potent, Well Tolerated, and Orally Active Protective Agent against Aminoglycoside-Induced Hearing Loss

Collagen immunostain

Novel mixed κ/μ receptor antagonist. having therapeutic potential for the treatment of depression and other stress-induced conditions

Negative allosteric modulator at the CB1 receptor

CB1 allosteric modulator

Selective p38alpha and p38beta kinase inhibitor

Lipoglycopeptide Antibacterial, acting as a inhibitor of Cytochrome P450 2C19/2C9, and a inducer of Cytochrome P450 3A4/2D6

Novel sodium/calcium exchanger (NCX) inhibitor

Novel potent dual orexin 1/2 receptor (OX1/2R) antagonist for the treatment of insomnia

Inhibitor of an enzyme responsible for the multidrug resistance phenotype in the yeast Saccharomyces cerevisiae.

Peripheral weak partial mu-opioid receptor agonist and a weak kappa-opioid receptor antagonist, preventing from being absorbed and entering the central nervous system

Second-generation taxane derivative with potential antineoplastic activity, binding to and stabilizing tubulin molecules, inhibiting cell division and cellular proliferation

Inhibitor of the influenza neuramidase enzyme, blocking neuraminidases on the surfaces of influenza viruses, interfering with host cell release of complete viral particles

Novel potent, orally efficacious, dual inhibitor of cMET and RON kinases

Novel cGMP phosphodiesterase (cGMP-PDE) inhibitor

Inhibitor of the glycan-processing enzyme endoplasmic-reticular glucosidase

Novel inhibitor of osteoclast differentiation through regulating MAPKs and Akt signaling pathways

Soluble secreted member of the tumor necrosis factor receptor superfamily, inhibiting osteoclastogenesis by interrupting the signaling between stromal cells and osteoclastic progenitor cells, leading to excess accumulation of bone and cartilage

Novel Inhibitor of Migration and Invasion of Osteosarcoma Cells Mediated by p53, Regulating EMT-Related Genes

Novel Inhibitor of Migration and Invasion of Osteosarcoma Cells Mediated by p53, Regulating EMT-Related Genes

Novel AMPK activator, inhibiting mTOR signaling and autophagy stimulation, activating mutations in RAS or BRAF

Novel potent inhibitor of the natural function of FDX1, promoting a unique form of copper-dependent cell death

Natural inhibitor of the Na+/K+-ATPase sodium-potassium ion pump

High affinity and human/rat species-selective histamine H3 receptor antagonist

Ovalbumin fragment peptide as a class I (Kb)-restricted peptide epitope, triggering T cell activation in immunology studies

Ovalbumin fragment peptide for study class II MHC-peptide binding and T-cell activation, binding to I-A(d) MHC class II protein, encompassing an allergenic and antigenic epitope of the ovalbumin protein

Narural broad anticancer agent, upregulating hsa-miR-155, suppressing the BCR-ABL fusion gene and dysregulating the PI3K/AKT/mTOR pathway

First-in-class small molecule potentiator of cancer virotherapy, significantly enhancing virus replication-associated luciferase expression specifically in the tumor

Novel anthelmintic agent, immobilising whipworm and reducing the ability of embryonated T. muris eggs to establish infection in the mouse host in vivo

Novel anthelmintic agent

Brain penetrant, selective and high affinity OX1R antagonist

Novel selective Ligand for the Orexin 2 Receptor (OX2R)

Potent inhibitor of PANC-1 cell migration and MYPT1 phosphorylation

Novel dual inhibitor of the p53 interaction with MDM2 and MDMX

PPARalpha/gamma agonist

Novel potent inhibitor of GVIA iPLA2 with little or no inhibition against GIVA cPLA2 (XI(50) = 0.0073 and >0.91, respectively)

Novel inhibitor of the bromodomain and extra terminal domain (BET) bromodomain family member BRD4(1)

Dual dopamine D2 and muscarinic M1 receptor ligand with putative antipsychotic and pro-cognitive potential

Novel inhibitor of human cathepsin L

Novel inducer of differentiation in all six AML cell lines

Novel sulindac derivative; anti-inflammatory and anti-cancer agent

Vasodilator and β-adrenoreceptor agonist

Antagonist of cell-surface heparan sulfate and heparin-protein interactions, reducing tau hyperphosphorylation and mitigating or delaying neuronal defects in tauopathies, including Alzheimer's disease

Synthetic hormone with anabolic and androgenic properties

δ-Opioid receptor agonist

Novel p18(INK4C) inhibitor

Novel INK4C inhibitor, specifically blocking the bioactivity of p18 protein

Novel INK4C inhibitor, specifically blocking the bioactivity of p18 protein

Novel INK4C inhibitor, specifically blocking the bioactivity of p18 protein

Second-generation active site-targeted covalent irreversible inhibitor of USP7

Novel potent inhibitor of mTOR activity, significantly suppressing macroscopic and histologic abnormalities associated with chemically-induced murine ulcerative colitis.

Novel P2Y1 Antagonist

Selective spleen tyrosine kinase (SYK) inhibitor, suppressing leukocyte immune function and inflammation, and leading to a reduction in arthritis score and attenuated histological damage

Novel modulator of p53 activity, arresting at G2/M phase inducing delay of cell cycle progression

Novel reactivator of mutant p53, fuctioning as a zinc metallochaperone (ZMC) with diminished copper binding that functions as a chemotherapy and radiation sensitizer

Novel inhibitor of atherogenesis and diabetes, significantly and specifically inhibiting αD-CEP binding

Novel bFGF antagonist peptide, inhibiting breast cancer cell growth

Neuroprotective agent, protecting ventral horn spinal cord motor neurons from cell death

Novel potent inhibitor of the AAA+ ATPase p97

Novel potent inhibitor of the AAA+ ATPase p97

Pseudomonas aeruginosa autoinducer

Novel partial agonist of peroxisome proliferator-activated receptor-γ (PPARγ), recruiting PPARγ-coactivator-1α, preventing triglyceride accumulation, and potentiating insulin signaling in vitro

Photoswitchable epithelial sodium channel (ENaC) blocker

Novel glutathione-S-transferase-p-activated nitric oxide donor, inhibiting proliferation and inducing apoptosis by targeting PI3K/AKT/mTOR and MEK/ERK pathways in hepatocellular carcinoma cells

Novel potent and selective inhibitor of protein arginine deiminase 3 (PAD3), having 15600 kinact/KI values and ≥10-fold selectivity for PAD3 over PADs 1, 2, and 4.

Partial DAT/5-HT transporter substrate

Full DAT/5-HT transporter substrate

Novel selective LYPLAL1 activator, increasing LYPLAL1’s catalytic activity likely by enhancing the efficiency of the catalytic triad charge-relay system, confering beneficial effects in a mouse model of diet-induced obesity

Full DAT/5-HT transporter substrate; Non-neurotoxic releasing agent of serotonin, norepinephrine, and dopamine; Full agonist at 5-HT2B and partial agonist at 5-HT2C

Potent dual dopamine-serotonin (DA/5-HT) releaser

Selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6

Novel Ras-Signaling Modulator, targeting acyl protein thioesterase 1 (APT1) and 2 (APT2) in cells

Potent serotonin-3 (5-HT3) receptor antagonist

Novel TLR2 agonist as potential adjuvant for cancer vaccines

Inhibitor of the Cell_cycle>cell cycle from G0/G1 to S phase with powerful antiparasite activity

Biological Active Reagents

Tamoxifen analogue; antiestrogenic

Novel potent pan-Raf and receptor tyrosine kinase inhibitor, potently inhibits all subtypes of Rafs with IC50 values of 3.49 (BRafV600E), 8.86 (ARaf), 5.78 (BRafWT), and 1.65 nM (CRaf), respectively

Potent and highly selective small molecule inhibitor of thioredoxin reductase (TrxR)

Pathway Preferential Estrogen, activating the extranuclear signaling pathway without activity on the nuclear signaling pathway

Blebbistatin derivative, increasing water solubility, decreases the inherent fluorescence, stabilizing the molecule to circumvent its degradation by prolonged blue light exposure, and decreasing its phototoxicity while retaining the in vitro and in vivo a

Isomer of CID-5951923

Selective cell-permeable inhibitor of non-muscle myosin II ATPases, being more stable and less phototoxic than Blebbistatin

Acetylcholinesterase inhibitor, the active metabolite of the insecticide parathion

Non-selective contact herbicide, killing green plant tissue on contact, being highly toxic and linked to Parkinson's disease, generating reactive oxygen species (ROS), which causes cell death and potentially leading to acute respiratory distress syndrome

Novel potent phosphodiesterase 3 inhibitor, suppressing the asthmatic response and showing both bronchodilating and anti-inflammatory effects

Novel potent phosphodiesterase 3 inhibitor, suppressing the asthmatic response and showing both bronchodilating and anti-inflammatory effects

Potent and Novel Dual PARP/BRD4 Inhibitor for Efficient Treatment of Pancreatic Cancer

Novel highly selective dual PARP1/BRD4 inhibitor (PARP1 IC 50 =49nM; BRD4 IC 50 =202nM), repressing the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells in vitro and in vivo

Novel Selective Cell-Active Inhibitor of PARP10

Fluorescent PARP1 Inhibitor for Glioblastoma Imaging

Natural ent-kaurane diterpenoid, markedly stimulates the expression of NKG2D ligands on hepatocellular carcinoma (HCC) cells, considerably enhancing their recognition and lysis by NK cells, covalently inhibiting peroxiredoxins I/II (Prxs-I/II) catalytic a

Novel antiviral agent, potently against Rabies virus (RABV) targeting host-rabies virus protein-protein interactions

Partial agonist at GABAA benzodiazepine receptors with sedative and anxiolytic effects

Novel potent inhibitor of

Novel potent glucosidase inhibitor, suppressing HCV virion assembly and secretion, potently inhibiting DENV infection in vitro

Novel Inhibitor of Parasite Proliferation of Asexual Blood Stage P. falciparum Parasites

Novel Inhibitor of Parasite Proliferation of Asexual Blood Stage P. falciparum Parasites

Novel enhancer of Th1 type cytokine production and primary T cell activation

Pyridobenzimidazole infraluciferin, an analog of D-luciferin, increasing bioluminescence activity while maintaining nIR bioluminescence

Novel αvβ3 inhibitor, showing excellent efficacy in a glioblastoma multiforme (GBM) mouse model

Novel dual inhibitor of the canonical and noncanonical NF-κB pathways, increasing the magnitude and duration of initial EGFR inhibitor response in multiple NSCLC models, decreasing PDHK1 expression, and suppressing phosphorylation of the PDHK1 protein sub

Novel calcineurin inhibitor in the C. albicans cells, enhancing susceptibility of the cells

Potent tubulin-binding agent with anti-tumor efficacy in hematologic cancers

Water-soluble novel potential COX-2 inhibitor

Non-dioxin-like (NDL) congener

Novel Chelator for Cu-64

Novel PSD95-nNOS inhibitor, disrupting the PSD95-nNOS interaction, attenuating neuropathic pain, decreasing SNL-induced spinal dorsal horn WDR neuron hyperexcitation

Novel activator of effector T cells, enhancing T cell proliferation and activation to release interferon gamma (IFN-γ) and interleukin-2 (IL-2) without blocking the programmed cell death 1 (PD-1)/programmed cell death-ligand 1 (PD-L1) binding and not dire

Novel α7 nAChR weak partial agonist, showing antinociceptive and anti-inflammatory properties

Organoselenium compound with antidepressant-like and memory enhancer actions

Potent antagonist of the series disrupting EphA2-ephrinA1 interaction, blocking EphA2 phosphorylation in prostate cancer cells at low

Highly selective α1L adrenaline receptor agonist

Novel potent dopamine D3R agonist (Ki=4.1nM)