Novel USP30 inhibitor, increasing Ub-TOM20 with an EC50 of 2.45 mM and inducing the maximal Ub-TOM20

Novel kidney urea transporter UT-A1 inhibitor

Novel

Quorum sensing modulator as a LasR antagonist

Non-immunosuppressive immunophilins ligand, demonstrating enhanced neuroregeneration in the peripheral nervous system and CNS

Novel Long Residence Time Superior Inhibitor of the Vasopressin V2 Receptor

Novel Mycobacterium Tuberculosis VapC-Activating Stapled Peptide, successfully penetrated Mycobacterium smegmatis cell membranes and exerted bactericidal activity at a minimum inhibitory concentration that inhibited 50% of the isolates (MIC50) < 6.25 μM

Novel potent inhibitor of FGFR4 kinase activity

Specific inhibitor of tissue Kallikrein>kallikrein

Selective 5-HT2C receptor full agonist

Orally acting antinociceptive muscarinic agonist

Prodrug of ganciclovir for treatment of cytomegalovirus (CMV) infection in those with HIV/AIDS or following organ transplant

Natural pseudo-aminosugar

Novel prodrug of luciferin to mimic the transport and activation of valacyclovir, , being a robust and functional determinant of VACVase activity

Novel selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), blocking VEGF-stimulated endothelial cell proliferation and migration and reducing tumor vessel permeability

Novel osteoclastogenesis inhibitor, preventing ovariectomy-induced osteoporosis in ddY mice

Partial α4ß2 nicotinic receptor agonist and α7 full agonist

Natural inhibitor of β-hexosaminidase release and tumor necrosis factor (TNF)-α secretion from rat basophilic leukemia (RBL 2H3) cells, with IC50 values of 10.4 μM and 16.8 μM, respectively, also inhibiting PKC β1 activity with an IC50 value of 36.2 μM

Novel anticryptosporidial agent, acting as a toll-like receptor-2 (TLR2) antagonist

Novel potent TLR‐4 activation inhibitor, attenuating the expression of fibrosis hallmark genes collagen, fibronectin (FN) and transforming growth factor β (TGF‐β) in kidneys and improved albumin/creatinine ratio with higher efficacy

Novel potent inhibitor of VDAC1, directly interacting with purified VDAC1 and reducing its channel conductance

Novel inhibitor of VDAC1 oligomerization and apoptosis

Novel non-nucleoside inhibitor of HCV RNA-dependent polymerase

Novel selective inhibitor of the γ-class enzyme of bacteria Vibrio cholerae A (VchCAγ)

Novel potent and selective CA IX inhibitor

Novel potent and selective CA IX inhibitor

Novel nonsecosteroidal vitamin D receptor (VDR) modulator, enhancing pancreatic cancer therapy through remodeling of the tumor microenvironment by combination with gemcitabine

Novel nonsecosteroidal vitamin D receptor (VDR) modulator, enhancing pancreatic cancer therapy through remodeling of the tumor microenvironment by combination with gemcitabine

Novel nonsecosteroidal vitamin D receptor (VDR) modulator, enhancing pancreatic cancer therapy through remodeling of the tumor microenvironment by combination with gemcitabine

Novel Aurora kinase inhibitor

Potent, Vascular Endothelial Growth Factor Receptor-​2 (VEGFR-2) Tyrosine Kinase Inhibitor

Activator for Proprietary Gene Therapy Promoter System

Serotonin-norepinephrine reuptake inhibitor (SNRI); Antidepressant

Novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupting Warburg metabolism and inducing context-dependent cytostasis in cancer cells

Antitumor agent

Natural Janus-Faced Modulator of Voltage-Gated Sodium Ion Channels, acting on the channel as either an agonist or antagonist depending on the nature of the electrophysiological stimulation protocol

Natural anti-inflammatory and antioxidant agent, inhibiting both iNOS expression and NO release in the LPS-induced J774.A1 macrophage cell line, enhancing protein expression levels of PARP-1 and p53, and attenuating intracellular ROS and stress (oxidative

Novel blocker of atrial potassium channels

Natural Reversible Plant Growth Inhibitor

Natural insect ryanodine receptor (RyR) antagonist

Apoptosis inducer, inhibiting Leiomyosarcoma and Malignant peripheral nerve sheath tumor growth

Potent inhibitor of acetylcholine transport

Novel anti-vesiculoviral agent, inhibiting transcription initiation of vesiculoviruses

Novel Inhibitor of the Pro-Angiogenic Activity of the Zinc Finger Transcription Factor Vezf1

The first sub-micromolar inhibitor of the VHL-HIF1α interaction

Natural protein kinase C (PKC) activator and HSP90 inhibitor, sensitizing human acute myeloid leukemia cells to tyrosine kinase inhibitor-induced myeloid differentiation via activation of PKC and upregulation of Lyn

Clopidogrel analog as an antiplatelet agent

Broad spectrum antibiotic, inhibiting adenylyl cyclase type 5 (AC5) and protecting against chronic coronary artery occlusion (CAO)

Selective long-acting beta2-adrenergic agonist (LABA) with inherent 24-hour activity for once daily treatment of COPD and asthma

Novel antagonist against hypocretin (orexin) receptor 2, significantly preventing acute morphine-conditioned place preference (CPP) and stress-induced reinstatement of extinguished morphine-CPP in mouse models of opioid reward and relapse

Natural inhibitor of 3C-like protease (3CLpro), targeting SARS-CoV-2 3CLpro, SARS-CoV 3CLpro and MERS-CoV 3CLpro

Natural antimicrobial, antioxidant, and anti-inflammator agent

Endogenous cannabinoid receptor mixed agonist/antagonist, being a full agonist at GPR55 and CB2 and partial agonist/antagonist at CB1

Natural inhibitor of ST2 (IL1RL1)

Coelenterazine analog for bioluminescence imaging (BLI)

Fluorescent cyclin-dependent kinase inhibitor, blocking the proliferation of human breast cancer cells

Novel and selective desensitizer of

Novel highly-selective melanocortin-4 receptor (MC4R) agonist, increasing resting energy expenditure in obese individuals

Novel potent VEGFR2 modulator, exhibiting increased antiangiogenic potency than voacangine against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects, resulting in significant tumor cell death in a mouse xenograft model

Novel calcineurin inhibitor and immunosuppressive agent

Novel potassium-competitive acid blocker

Novel potent and highly selective type-II inhibitor of p38α/β, targeting an inactive state of the kinases induced by a unique folded P-loop conformation

Potent Antiandrogen, Targeting the BF3 Site of the Androgen Receptor and Inhibiting Enzalutamide-Resistant Prostate Cancer

Novel potent and selective inhibitor of ERα-dependent cell growth and gene expression, preventing the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner

S1P1/S1P3 receptor agonist

Novel Androgen Receptor Antagonist, inhibiting the LNCaP cell line as well as cell lines with wild-type androgen receptor

Competitive S1P1/3 antagonist, increasing capillary permeability as measured by Evans blue dye leakage in mouse lung tissue

Corrector of F508del-cystic fibrosis transmembrane conductance regulator (CFTR) mutant

Inhibitor of the catalytic activity of VRV-PL-VIIIa, strongly inhibiting the hemolysis of red blood cells and VRV-PL-VIIIa-induced myotoxicity and lung hemorrhage in mice

Novel Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)

Novel inhibitor of geranylgeranyl diphosphate synthase (GGDPS)

Novel Promoter of Neuronal Branching Via Transcellular Activation of the Focal Adhesion Kinase (FAK) and the ERK1/2 Signaling Pathway In Vitro

Sphingosine kinase (SphK) inhibitor, having modest SphK2-selectivity

Novel selective agonist of TLR8

Novel non-MPEP site metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs)

Selective modulator of G protein-coupled inward rectifier K (GIRK)

Allosteric modulator of the M1 muscarinic receptor

Novel Positive Allosteric Modulator (PAM) of the Metabotropic Glutamate Receptor 5 (mGlu5)

Novel Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5, Revealing Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

Potent and specific PAM for the rat mGluR5 receptor

Potent noncompetitive antagonist of Metabotropic_glutamate_receptor_5>metabotropic glutamate receptor 5 (mGlu5)

VU0366248 is a mGlu5 negative allosteric modulator.

Novel Positive Allosteric Modulator (PAM) of the Metabotropic Glutamate Receptor 5 (mGlu5)

Highly potent non-MPEP site metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM)

Muscarinic antagonist; inhibiting ACh-induced Ca(2+) responses at rat M(1-5) receptor subtypes

Novel positive allosteric modulator (PAM) of mGlu4

Allosteric modulator of the M2/5 muscarinic acetylcholine receptor

Highly M1-selective antagonist

Novel M4 muscarinic acetylcholine receptor modulator

Novel mGlu4 positive allosteric modulator (PAM)

Novel negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

Highly selective muscarinic M1 PAM

Selective orthosteric M1 antagonist

Novel, CNS Penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) Positive Allosteric Modulator (PAM)

Novel potent and selective metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM)

Potent and selective mGlu5 negative allosteric modulator (NAM)

Novel potent mGlu4 PAM with an attractive DMPK profile, and robust efficacy in preclinical Parkinsons disease model, haloperidol-induced catalepsy (HIC)

mGlu1 positive allosteric modulator (PAM)

Novel cyclooxygenase-1 (COX-1)-selective inhibitor

Novel modulator of mammalian inward rectifying potassium (Kir) channels

Novel selective negative allosteric modulator (NAM) of metabotropic glutamate receptor subtype 2

Novel potent and highly selective mGlu1 PAM (22nM), reducing striatal DA release in vivo and displaying antipsychotic efficacy

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel M4 positive allosteric modulator (PAM)

Novel CNS penetrant pan-muscarinic antagonist

Novel PAM of Group III (mGlu4/6/7/8) mGlu receptors

Novel selective mGlu3 NAM, showing efficacy in tail suspension, elevating zero maze and marble burying, suggesting selective inhibition of mGlu3 affords anxiolytic-like and antidepressant-like phenotypes in mice

First-in-class selective mGlu7 positive allosteric modulator (PAM), displaying CNS penetration in both mice (Kp = 2.74) and rats (Kp= 4.78)

Potent histamine H3 receptor silent antagonist

Novel full inverse agonist at CXCR3 N3.35A

Potent H4R ligand

Novel potent ligand at 5-HT3A and 5-HT3AB receptors with different activities

VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity.

Potent human H4 receptor inverse agonist

Highly Potent Human Histamine H4 Receptor Inverse Agonist

Potent CXCR3 Antagonist, extending from the minor pocket into the major pocket of the transmembrane domains and binding between residues in helices 1 (Y1.39), 2 (W2.60), 3 (F3.32), 4 (D4.60), 6 (Y6.51), and 7 (S7.39, Y7.43)

First reported nonpeptidomimetic agonist on The G protein-coupled chemokine receptor CXCR3

Partial agonist in hH 4 R-mediated G protein signalling and β-arrestin2 recruitment, bounding covalently to the hH4R

Novel robust and fatigue-resistant photoswitchable GPCR antagonist

Novel robust and fatigue-resistant photoswitchable GPCR antagonist

Novel inhibitor of Hbp secretion, activating σE stress, impairing Hbp secretion and decreasing the abundance of OMPs, consistent with impaired BAM function

Novel photoswitchable modulator of the CXCR3 chemokine receptor

Novel CXCR3 ligand, photoswitching from antagonism to agonism

Novel photoswitchable modulator of the CXCR3 chemokine receptor

Histamine H3 receptor antagonist

H3R inverse agonist

Adenosine A3 receptor (A3AR) allosteric modulator

Novel full inverse agonist at CXCR3 N3.35A

Full agonist of hH4R with ~300-fold selectivity over hH3R and hH2R, but showing potent inverse agonistic activity at hH1R

Potent histamine H4 receptor full agonist

Allosteric modulator of A3 adenosine receptors

Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.

Novel Probe of Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity

W-13 hydrochloride is a calmodulin antagonist. W-13 hydrochloride can inhibit Tamoxifen (HY-13757A)-resistant human breast cancer cell growth.

Calmodulin antagonist, inhibiting Ca2+/calmodulin-regulated enzyme activities

Mixed competitive/noncompetitive inhibitor of

Nocel inhibitor of BMI1 promoter activity, decreasing BMI1 protein levels in HCT116 human colon carcinoma cells, significantly reducing levels of the CSC biomarker epithelial cell adhesion molecule and diminishing the self-renewal capability of CSCs

Very late adhesion molecule 4 (VLA-4) antagonist, inhibiting VLA-4/VCAM-1 ligation as a means of modulating eosinophil functions beyond its action on cell adhesion and migration

SGLT2 inhibitor

ATP-sensitive potassium channel opener

Inhibitor of human collagenase-3 (MMP-13)

Potent and selective inhibitor of matrix metalloprotease MMP-13 (Collagenase-3)

Inhibitor of matrix metalloproteinase-1 (MMP-1)

Potent and Selective Inhibitor of the Norepinephrine Transporter

Secreted frizzled-related protein-1 (sFRP-1) modulaitor

Novel inhibitor of The epidermal growth factor receptor (EGFR), decreasing NSCLC cell proliferation and colony formation, by causing G2/M arrest and apoptosis.

Non-peptide GLP-1 receptor agonist, blocking inflammatory nociception by stimulating β-endorphin release from spinal microglia

Novel Inhibitor of PBP2, Showing Potent β-Lactam Enhancer Activity against Pseudomonas aeruginosa, Including Multidrug-Resistant Metallo-β-Lactamase-Producing High-Risk Clones

Highly conserved neuropeptide derived from Chromogranin A (Parathyroid Secretory Protein 1)

Novel very potent and long acting hetrazepinoic PAF-antagonist

Novel inhibitor of type III secretion system ATPase EscN from enteropathogenic Eecherichia coli

Novel fluoroquinolone antibiotic with potent antimicrobial activity, showing the potential to overcome major drug resistance; its antimicrobial activity was less affected by both pump-mediated efflux and QRDR mutations in P. aeruginosa compared with LVX a

Novel Anti-malarial Plasmodium-Selective Proteasome Inhibitor

Dopamine reuptake inhibitor, also having some SERT affinity

B2 bradykinin receptor antagonist

Natural potent antitumoragent, targeting sarco/endoplasmic reticulum calcium-ATPase (SERCA)2

Novel dual inhibitor of histone deacetylase and topoisomerase I

Novel potent dual inhibitor of phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR), preventing PI3K signaling and inhibiting the proliferation of transformed cells with oncogenic PI3K mutant

Novel GluN2B-specific NMDAR antagonist, completely preventing the decrease in insulin secretion of about 32 % provoked by a 24-h-treatment with NMDA/glycine, eliminating NMDA-induced changes in the oxidation status of the islet cells and elevating the sen

Potent uncompetitive NMDA receptor antagonist

Unique neuroprotectant against oxidative injury, being a highly promising remedy for the treatment of amyotrophic lateral sclerosis (ALS)

Novel Allosteric WNK Kinase Inhibitor

Novel potent dual inhibitor of Wnt and hedgehog signalings, blocking porcupine and smoothened

Novel dual BRD4 and PLK1 inhibitor (IC 50 values of 109 and 22 nM, respectively), showing strong antiproliferative activity against cancer cells

Novel GPR52 agonist, dose-dependently inducing elevation of intracellular cAMP in HEK293/GPR52 cells

Novel inhibitor of the JAK2/STAT3 pathway

Main active metabolite of tazanolast, inhibiting dose-dependently compound 48/80-induced histamine release from rat peritoneal mast cells

Novel Dual Inhibitor of Nitric Oxide and Prostaglandin E2 Production

Potent inhibitor of Plasmodium falciparum dihydrofolate reductase (DHFR)

Novel potent inhibitor of Schistosoma mansoni cathepsin B1 (SmCB1) with IC50 ~0.6 nM

Novel potent inhibitor of Schistosoma mansoni cathepsin B1 (SmCB1) with IC50 ~0.2 nM

Analog of K11777; Irriversible effective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777.

Novel potent RET kinase inhibitor with >500-fold selectivity against KDR (Kinase insert Domain Receptor) in cellular assays

Novel highly potent and orally active ABCB1 modulator capable of overcoming MDR, stabilizing ABCB1 by directly binding to ABCB1, stimulating the activity of ABCB1 ATPase without inhibitory activity against CYP3A4, increasing the sensitivity of SW620/Ad300

Novel xanthine oxidase inhibitor

Simplified analog of the selective Gαq/11 inhibitor YM-25489

Novel α/ß-hydrolase domain 6 (ABHD6) inhibitor

Novel urokinase inhibitor

Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR)

Potent inhibitor of proliferation activity against a broad spectrum of human cancer cell lines, induces G2/M phase arrest and apoptosis through the PI3K/Akt pathway

Natural antibacterial agent against Gram-positive bacterial pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), Enterococcus faecium and Enterococcus faecalis

Antibiotic, exhibiting strong antibacterial activities and showing potent cytotoxicity, inhibiting HSP47 gene expression produced by Streptomyces sp

Novel antibiotic, showing 3- to 10-fold greater cytotoxicity than Xantholipin against a select panel of human cancer cell lines, demonstrating powerful antimicrobial activity against both Gram-positive bacteria and fungi

Quantity (mg or Unit) Unit Price ($/mg or $/Unit) Final Price 100 $26.55 Total: $2,655.00 50 $30.68 Total: $1,534.00 25 $35.99 Total: $899.75 10 $42.48 Total: $424.80 5 $50.15 Total: $250.75

Novel PKM2 activator

Potent and Selective Stearoyl-CoA Desaturase-1 Inhibitor

Novel INK4C inhibitor, specifically blocking the bioactivity of p18 protein and promoting human and murine hematopoietic stem cell ex vivo expansion

Novel non-coding RNA prototype Xist ligand, specifically binding the RepA motif of Xist, reducing the conformational space of RepA, displacing cognate interacting protein factors (PRC2 and SPEN), suppressing histone H3K27 trimethylation, and blocking init

Novel dual inhibitor of AF9 and ENL YEATS domains

Novel Potent Pan-Filovirus Inhibitor, showing potent inhibition against infectious EBOV Zaire (0.09 μM) and MARV (0.64 μM)

Novel Akt1/2 inhibitor

Potent modulator of P-glycoprotein-mediated multidrug resistance (MDR), inhibiting the binding of cytotoxics to P-glycoprotein

Novel selective β-catenin degrader

Carbonic anhydrase inhibitor; Fungal metabolite

Novel activator of p21 promoter in a p53-independent manner

Novel TRIM24/BRPF1 dual inhibitor with IC 50 values of 0.98 and 1.16 μM, respectively

Novel non-peptidic highly potent, soluble and selective NPY Y2 antagonist

Novel, selective, soluble non-​peptidic NPY Y2 receptor antagonist with enhanced CNS exposure

Selective Rho-associated kinase (ROCK) inhibitor