Cytotoxic MDR-selective ligand

Novel anticancer agent, suppressing the growth of several cell lines derived from lung, colon, breast, ovarian, and kidney cancers

Novel down-regulator of EZH2, inducing G2/M cell-cycle arrest of cancer cells and degradating p53 via proteasome-dependent and -independent pathways

Telomerase inhibitor, stabilizing G-quadruplex and suppressing cell growth of A549 human lung cancer cells through activation of the ATR/Chk1-dependent pathway

Telomerase inhibitor, anticancer agent

Novel inhibitor of poly (ADP-ribose) polymerase-1 (PARP-1)

Novel inhibitor of lipid metabolism, disrupting tubulin polymerization,suppressing monoglycerol metabolism depleting lipids and inhibiting the growth of both lymphoma and RCC both in vitro and in vivo

The first reported BoNT/E small molecule inhibitor

Novel inhibitor of nucleoside hydrolase (NH)

Selective inhibitor of HsEg5

Potent inhibitor of endopeptidase activity of botulinum neurotoxin type A light chain (rBoNT/A-LC)

Tyrosyl-DNA phosphodiesterase (Tdp1) inhibitor

First-in-class probe of Rad6 function, inhibiting Rad6 function and Rad6-Rad18 interaction in the PCNA ubiquitination cascade

Novel B-Raf(V600E) inhibitor

Novel stimulator of neurogenesis of human hippocampus-derived neural stem cells in vitro and in vivo.

Novel inhibitor of neutral sphingomyelinase 2 (nSMase2) for the treatment of neurodegenerative diseases

Novel free radical scavenger, against light-induced photoreceptor cell damage

Potent anti-HBV agent, targeting the NTCP-APOA1-HBx-Beclin1-mediated autophagic pathway

Novel nonpeptide selective ligand for NTS2

Novel nonpeptide potent and selective partial agonist of the Neurotensin receptor type 2 (NTS2)

Novel Allosteric Modulator of RNA Binding Targeting the N-Terminal Domain of TDP-43

The first NTR-responsive PROTAC, incorporating the caging group on the Von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand, efficiently degrading the EGFR protein and subsequently exert antitumor efficacy

Novel potent STAT3 inhibitor, exhibiting much improved in vivo pharmacokinetic parameters in rats and efficacies against proliferations in multiple cancer cell lines

Novel potent STAT3 inhibitor

Novel potent and selective non-thiazolidinedione partial Peroxisome_proliferator-activated_receptor>PPARγ agonist, acting as an antibiotic effectively against bacterial persisters

Novel potent CDK2 inhibitor

Novel DNA methytransferase inhibitor, be significantly safer and more effective than decitabine in xenograft models of human leukemia and colon cancer

Novel highly potent and selective MEK4 inhibitor

Novel potent activin antagonist

First-in-class activin antagonist, specifically binding to ALK4, which opens a completely new approach to inhibiting the activity of TGF-beta receptor superfamily members

Nucleosidic antibiotic

Novel inhibitor of Helicobacter pylori , targeting H. pylori's respiratory complex I subunit NuoD

Novel Potent Cell-Active Inhibitor of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition

Novel Inhibitor of the NusB-NusE Protein-Protein Interaction with Antibiotic Activity

Novel modulator of the NusB-NusE interaction

p53-MDM2 binding inhibitor; p-Glycoprotein (p-gp) transport substrate; Antitumer agent

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