Antibacterial agent, with a relatively narrow spectrum against bacteria and a very high CC 50 value

Novel specific inhibitor of HA-mediated viral entry, inhibiting HPAI H5N1 virus strain A/Hong Kong/H5N1

Topical nonnucleoside reverse transcriptase inhibitor, partially preventing vaginal RT-SHIV infection of macaques

Potent and HDAC class I-selective inhibitor

Novel potent acetylcholinesterase (AChE) inhibitor

The first inhibitor of forkhead Box Protein C2 (FOXC2)

Novel selective PARP1 inhibitor, inhibitng apoptosis and blocking poly ADP-ribosylation of histone H1 in hydrogen peroxide treated SH-SY5Y neuroblastoma cells

Novel hybrid retinoid-HDAC inhibitor

Potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively)

Novel neurotropic agent

Specific and highly fluorescent substrate for caspase-1, also acting as a substrate for caspase-4

Novel selective inhibitor of the Polo-box domain of Polo-like kinase 1 (PLK1)

First-in-class inhibitor of MFS efflux pump CaMdr1p

Novel inverse agonist for the pancreatic-type ATP-sensitive K channel as vascular relaxing agent

Potent and selective inhibitor of NLRP3, reducing interleukin-1β (IL-1β) production in vivo and attenuating the severity of experimental autoimmune encephalomyelitis (EAE)

Albumin-binding prodrug of Doxorubicin

Novel potent F508del-CFTR corrector, modulating poly-ADP ribose polymerase 3 and poly-ADP ribose polymerase 16 activities

Selective NA reuptake inhibitor with 5-HT3 receptor antagonism

Novel inhibitor of p53-MDM2 interaction

Novel potent and selective degrader of Mcl-1

Novel reversible covalent inhibitor for Mcl-1 with improved water solubility than Mcl-1 Inhibitor-5

Novel selective Mcl-1 inhibitor

The first reversible covalent inhibitor for Mcl-1, a protein-protein interaction (PPI) target

Novel potent and selective inhibitor of the apoptosis regulating proteins Mcl-1

Novel mc (maleimidocaproyl) linker plus MMAD (Monomethylauristatin D) to be used for prepare antibodies conjugates via cysteine-capped mechanism

Novel highly selective inhibitor of monocarboxylate transporter 4 (MCT4/SLC16A3), resulting in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells

Novel SARS-CoV-2 Main Protease (Mpro) inhibitor, binding to Subsites S1 and S2 (Kd=1.3 µM)

First-in-class highly potent PROTAC degrader of MDM2

Diuretic agent, impling an increase in the Na+ excretion and showing antihypertensive effect

Novel valproic acid (VPA) derivative, as a potent STAT3 inhibitor

Novel partial PPARgamma ligand, displaying partial agonist activity in biochemical and cell-based transactivation assays, and reversed insulin resistance

Novel proteolysis-resistant self-localizing ligand (SL), sustaining PM localization of eDHFR-fusion proteins (over several hours to a day), inducing prolonged signal activation and cell differentiation

Novel MC5R antagonist

Novel potent and highly selective melanocortin-3 receptor (MC3R) agonist, showing greater than 140-fold selective for the mMC3R over the mMC4R, possessed 70 nM potency at the mMC3R, and partially stimulated the mMC4R at 100 μM concentrations without antag

Novel potent and nonselective MC3R and MC4R macrocyclic agonist. decreased food intake and respiratory exchange ratio (RER)

Novel Inhibitor of BAF, activating latent HIV-1

Novel peroxisome proliferator activated receptor

Novel peroxisome proliferator activated receptor γ (PPARγ) ligand

Dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase

Potent Peptide dual inhibitor of MDM2/X, inhibiting p53 interactions with MDM2 (IC50 = 10 nmol/L) and MDMX (IC50 = 100 nmol/L), inducing apoptosis and cell cycle arrest of cell lines with overexpressed MDM2/X

Novel potent dual MDM2/XIAP inhibitor

Novel inhibitor of the MDM2-p53 interaction

Potent ligand of the central CB1 receptor

Novel selective inhibitor of succinate dehydrogenase (complex II) of dermatophyte species

Potent and efficacious mobilizing agent of hematopoietic stem and progenitor cells (HSPCs), activating MMP-9 expression and disrupting the SDF-1α/CXCR4 axis, exhibiting more significant mobilizing effects than G-CSF or AMD3100

Second generation papaverine analog, acting as an anticholinergic agent

Selective FXR antagonist, ameliorates glucose homeostasis in type 2 diabetic mice

Polyketide antibiotic, acting as a AKT selective kinase inhibitor, alkylating a regulatory loop cysteine

Progestational hormone, for the treatment of menstrual irregularities, prostatic hypertrophy, and endometrial carcinoma

Potent sPLA2 inhibitor, having no effect on arachidonic acid release and platelet activating factor synthesis

Inducer of Megakaryocyte Differentiation in Erythroleukemia Cells, Impairing Bcr-Abl Signaling Cascades

Natural dual inhibitor of COX-2 and EGFR, improving program death 1 (PD-1) checkpoint blockade therapy through normalizing tumor vasculature and PD-L1 downregulation

Prodrug of melarsen oxide (Mel Ox), irreversibly binding to vicinal sulfhydryl groups on pyruvate kinase, disrupting energy production in the parasite

Inhibitor of cholesterol esterification

Novel Multi-Kinase Inhibitor, Triggering Mitotic Catastrophe of Glioma Stem Cells Mainly through MELK Kinase Inhibition

Potent, selective and orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4)

5-HT2A/D2 receptor antagonist

Novel potent and selective nonpeptide kinin B2 receptor antagonist

Novel Cell Death-Inducing Kinase Inhibitor with Enhanced Selectivity for Cyclin-Dependent Kinases; Antimalarial

Potent cell-permeable, ATP site-targeting inhibitor of CDKs

Potent cell-permeable, ATP site-targeting inhibitor of CDKs

Apoptosis inducer, triggering ROS dependent autophagy-associated apoptosis in a variety of human cancer cell lines and against mutant KRAS expressing cancer cells involving AKT-dependent ROS production

LXR-α antagonist, inhibiting hepatic lipid accumulation by activating AMP-activated protein kinase in human HepG2 cells

Anabolic and androgenic agent

Novel selective and potent full KOP receptor agonist with fewer side effects (e.g., sedation or anhedonia) than classic KOP receptor

Novel selective GPR120 agonist

Cyclooxygenase 3 (COX3) inhibitor, acting as a potent inductor of cytochrome P450 isoenzymes CYP2B6 and CYP3A4

Potent, long-lasting, and selective antagonist of morphine-mediated antinociception

Natural potent anti-proliferative agent, inducing apoptotic cell death

Inhibitor of pro-inflammatory mediator release from mast cells

Useful pharmaceutical building block

Novel photosensitizer as a photodynamic antimicrobial agent against Staphylococcus aureus, Escherichia coli, Candida albicans, and Methicillin-resistant S. aureus (MRSA)

Novel inhibitor of ABCG2 transporter function

Natural antifungal agent, significantly inducing lipid peroxidation, activating the antioxidant enzymes, and exhibiting effective activity against F. solani (EC50 = 10.56 µM)

Metablite of PRIMA-1 and APR-246, covalently binding to cysteine residues in mutant p53 and wild type p53, and being increased in unfolded p53, inducing massive apoptosis in p53 null tumor cells

Novel Class of Cannabinoid CB2 Receptor Inverse Agonist

Peripherally restricted μ-opioid antagonist

Highly Selective Class II MET Inhibitor

Dopamine D2 antagonist, antiemetic

Non-depolarizing muscle relaxant

Radiographic Contrast Agent

Novel Dual Fluorescent and Magnetic Resonance False Neurotransmitter

Novel potent negative allosteric modulator (NAM) of mGlu2

Novel potent inhibitor of the p53-MDM2 interaction with an IC50 value of 67.5 nmol/L, against acute leukemia cell lines with different p53 status and was much less effective in inducing MDM2 degradation

mG2N001 is a potent negative allosteric modulator (NAM) of metabotropic glutamate receptor 2 (mGluR2) with IC50 of 93 nM.

Novel, multi-targeted kinase inhibitor, demonstrating potent inhibition of Trk, RET and DDR, in addition to Met, Axl and VEGFRs

Selective metabotropic glutamate 2/3 receptor agonist

Potent and orally active group II mGluR antagonist with antidepressant-like potential

Near-infrared cyanine dye, acting as an optical imaging agent

Novel photodynamic antitumor agent

Novel tyrosinase inhibitor, showing concentration-dependent inhibitory effects with no significant cytotoxicity in cell viability assay

Novel potent HDAC inhibitor, possessing potent anticancer activities

Novel potent histone deacetylase (HDAC) inhibitor, inducing apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells

Novel topoisomerase II inhibitor, markedly inducing apoptotic cell death via the mitochondria-mediated intrinsic pathway in LNCaP cells

Novel tyrosinase inhibitor, down-regulating of MITF and tyrosinase through direct tyrosinase inhibition

Novel sensitizer of cancer cells, significantly increasing DNA damage as determined by DNA breakage, levels of damage-responsive proteins, and DNA foci

Novel inducer of G2/M phase arrest in the cell cycle progression, resulting in growth inhibition and induction of apoptosis in a concentration-dependent manner, and inhibition of proliferation in a time-dependent manner

Novel inhibitor of nitric oxide-induced melanogenesis, targeting the NO-induced cGMP signaling pathway

Novel tyrosinase inhibitor, directly inhibiting mushroom tyrosinase

Novel tyrosinase inhibitor, suppressing UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress

Novel Chemically Stable, Potent, and Efficacious MDM2 Inhibitor

Novel inhibitor of TMPRSS2, also strongly preventing SARS-CoV-2 multiplication and CPE in Calu-3 cells in a dose-dependent manner. causing strong inhibition of SARS-CoV-2 replication

Novel MDM2 antagonist, restoring p53 functions and increases the life span of orally treated follicular lymphoma bearing animals

Novel matriptase-1/matriptase-2 (MT-1/2) inhibitor, also inhibiting TMPRSS2, proteolytic activation and multiplication of influenza A virus in Calu-3 cells

Highly Potent and Efficacious MDM2 Inhibitor

Novel inhibitor of microtubule assembly, inducung mitotic arrest and apoptosis of MM cells

Novel Potent MIF Degrader

Immunomodulator, regulating the activation of monocytes and macrophages, upregulating the secretion of pro-inflammatory cytokines such as TNF-alpha, IL-1, IL-8, nitric oxide and prostaglandins E2 and D2

Novel inhibitor of Migration-Inducting Gene 7 (MIG-7) expression, suppressing EOC cell growth and VEGFA expression

Product Description:

MAO-B inhibitor and glycine prodrug, being studied for treatment for the symptoms of Alzheimer's disease

Natural anti-tumor agent, demonstrating with tumor inhibitory efficacy comparable or even superior to the mainstay chemotherapeutics paclitaxel or fluorouracil

First-in-class inhibitor of MYC-induced nuclear antigen (MINA53) with selectivity over NO66 and other JmjC oxygenases

Inhibitor of cholecystokinin B receptors (CCK2)

Novel inhibitor of the prostate-specific membrane antigen (PSMA)

Novel inhibitor of the prostate-specific membrane antigen (PSMA)

Novel long-lasting myostatin inhibitor, significantly increasing muscle mass and hindlimb grip strength in Duchenne muscular dystrophic model mice

Novel photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor

Novel selective positive allosteric modulator (PAM) at the M1 muscarinic acetylcholine receptor

Novel thapsigargin-based PSMA-activated prodrug, inhibiting the sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump protein

Novel specific and efficient inhibitor of miR-21 expression, inducing a 485% increase in the luciferase reporter signal at 10 μM

Novel inhibitor of microRNA-21 (miR-21)

Novel Miro1 degrader, rescuing dopaminergic neurodegeneration and promoting Miro1 degradation in Parkinson’s Disease fibroblasts

Novel degrader of Miro1 (mitochondrial Rho GTPase 1), reducing Miro1 levels in fibroblasts and stress-induced degeneration of dopaminergic neurons derived from Parkinson's disease (PD) patients, as well as age-dependent neuronal loss and prolongs lifespan

Novel inhibitor of AMA1-RON2 interaction, blocking merozoite invasion from schizont-infected RBCs; Antidepressant; Acetylcholinesterase inhibitor

The first small molecule inhibitor of Mitf-E-box DNA binding with depigmenting activity

Sensitive and specific Raman probe for live cell imaging of mitochondria

Fluorescent probe for measuring the activity levels of erasers of S-palmitoylation, acyl-protein thioesterases (APTs), within mitochondria of live cells

Radiation Mitigator, reducing lipid hydroperoxides and preventing apoptotic cell death

Novel mitochondrial-targeted pan-APT inhibitor

Novel potent antiproliferative mitochondria-targeted OXPHOS inhibitor (IC50=38 nM) in MiaPaCa-2 cells, being more effective than other inhibitors of OXPHOS in MiaPaCa-2 and U87MG cells

Novel selective fluorescent H2O2 probe, tracking the mitochondria of live biological specimens and responds to local fluxes of hydrogen peroxide (H2O2) by a turn-on fluorescence enhancement

Antineoplastic DNA alkylating agent

Specific inhibitor of the cellular inosine-5-monophosphate dehydrogenase (IMPDH); Immunosuppressive agent

Potent and selective PDE4 inhibitor

Novel potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R)

The class III antiarrhythmic agent, blocking HERG, a human cardiac delayed rectifier K+ channel

Novel Dipeptidyl peptidase IV (DPP-4) inhibitor, improving neovascularization by increasing both the number of circulating endothelial progenitor cells and endothelial nitric oxide synthetase expression

Potent and Selective 5-Lipoxygenase Inhibitor

Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Novel Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure

Novel renin inhibitor

Potent TRPV1 antagonist

Potent and selective human type-1 5alpha-reductase inhibitor

Novel Selective Androgen Receptor Modulator (SARM)

Novel nonpeptide bombesin receptor subtype-3 agonist

Novel potent muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM)

Novel bombesin receptor subtype-3 (BRS-3) modulator

Novel liver-targeting inhibitor of stearoyl-CoA desaturase (SCD)

Novel agonist of G-protein coupled receptor 40 (GPR40)

Prodrug of raltegravir with enhanced colonic absorption

Novel potent and selective MKK3/6 inhibitor

Novel highly specific, potent, orally bioavailable MKP5 inhibitor

Novel endoplasmic reticulum proteostasis modulator, enhancing insulin production in pancreatic β cells, inhibiting the UPR, alleviating ER stress and protein aggregation, improving intracellular insulin levels and insulin secretion

Novel Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake

Selective inhibitor of Myosin Light Chain Kinase (MLCK)

Novel IKK2 inhibitor, decreasing NF-κB activation and down-regulating the expression of a number of inflammatory proteins

Novel potent DNA binding agent, stabilizing topoisomerase-dependent cleavage, demonstrating exceptional efficacy against a number of murine and human tumor models

Second generation 5-LO inhibitor, blocking the production of leukotrienes

Novel selective and potent inhibitor of recombinant h12/15-LOX and cellular mouse 12/15-LOX (m12/15-LOX)

Potent and selective competitive inhibitor of human epithelial 15-lipoxygenase-2 (15-LOX-2)

Potent and selective mixed-type inhibitor of human epithelial 15-lipoxygenase-2 (15-LOX-2)

Novel potent inhibitor of EBOV infection

Novel Inhibitor of Human Cytomegalovirus

Potent inhibitor of STAT3 and Akt signaling

Novel dual JAK/Src kinase inhibitor, suppressing growth of diverse cancer cells

Novel inhibitor of human cytomegalovirus (HCMV) infection

Potent agonist of TRPML channels specifically activating lysosomal ML1 currents

Novel potent and selective MALT-1 protease inhibitor, showing improved solubility and permeability in comparison with MLT-748

Novel potent IDO1 inhibitor, showing low cytotoxicity and higher selectivity for IDO1 over TDO enzyme

Novel potent and selective HDAC8 inhibitor

Novel potent and selective HDAC8 inhibitor

Novel potent and selective HDAC8 inhibitor

Novel highly potent and selective MMP13 inhibitor

Negative allosteric modulator (NAM) ligand for the mGlu5 receptor

Novel Mmpl3 inhibitor, indirectly blocking translocation of Trehalose Monomycolates across the IM

Highly water-soluble antifibrotic agent, reducing the profibrotic phenotype induced in vitro in primary human fibroblasts and ameliorating bleomycin-induced pulmonary fibrosis in vivo

Novel inhibitor of lanosterol-14-alpha-demethylase (TcCyp51)

The first small-molecule anti-plasmodial agent, disrupting rosetting, simultaneously restoring microcirculation and reduce parasite load

Novel antimalarial agent against asexual stages of P. falciparum

Novel potent Plasmodium lactate transporter PfFNT

Novel MEP pathway-targeting antimalarial agent

Novel antimalarial agent with increased efficacy against one or more pfatp4 mutated clones

Novel Inhibitor of Plasmodium falciparum

Novel antischistosomal agent against chronic S. mansoni infection

Novel antischistosomal agent against chronic S. mansoni infection

Novel antimalarial agent with increased efficacy against one or more pfatp4 mutated clones

Novel inhibitor of Plasmodium falciparum, killing both blood- and sexual-stage P. falciparum parasites

Novel antimalarial agent against Plasmodium falciparum

Novel antimalarial agent, targeting P. falciparum farnesyltransferase PfFT, showing remarkable growth inhibition with EC50 value of 0.4 µM and presenting good selectivity index (SI > 250)

Selective allosteric inhibitor of Plasmodium Kinesin-5

Novel potent inhibitor of P. falciparum asexual blood stages, inhibiting heme detoxification

Novel potent broad antiparasitic agent against intracellular Leishmania amastigotes, Trypanosoma brucei, and Plasmodium falciparum

First-in-class acetyl-CoA synthetase (AcAS) inhibitor, showong single digit nanomolar in vitro activity against P. falciparum and P. vivax clinical isolates, and potently blocking P. falciparum transmission to Anopheles mosquitoes

Novel anticancer agent, inducing apoptosis, inhibiting migration and invasion

Novel highly potent and selective MNK1/2 kinases inhibitor

Potent and selective Mnk2 inhibitor

Cell-permeable superoxide dismutase (SOD) mimetic

Novel inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity