E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively.

Nemorubicin, also known as PNU152243A, is a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail. Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases.

Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

ITK inhibitor (CAS 439574-61-5 ) is a Interleukin-2-inducible T-cell kinase (Itk) inhibitor..

CZh226 hydrochloride (CZh-226) is a potent, selective inhibitor of p21-activated kinase 4 (PAK4) with Ki of 9 nM, displays 346-fold selectivity over PAK-1.

UC-764864 (UC764864) is a small-molecule inhibitor that targeted ubiquitin-conjugating enzyme UBE2N active site.UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.Inhibition of UBE2N function disrupted oncogenic immune signaling by promoting cell death of leukemic HSPCs while sparing normal HSPCs in vitro.

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.

VMAT2 ligand, stimulating dopamine release, inhibiting the reuptake of dopamine and serotonin, acting as a mixed agonist-antagonist at nicotinic acetylcholine receptors and antagonist at µ-opioid receptors

Tazobactam inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups. It is commonly used as its sodium salt, tazobactam sodium. Tazobactam is combined with the extended spectrum β-lactam antibiotic piperacillin in the drug piperacillin/tazobactam, one of the preferred antibiotic treatments for nosocomial pneumonia caused by Pseudomonas aeruginosa.[medical citation needed] Tazobactam broadens the spectrum of piperacillin by making it effective against organisms that express β-lactamase and would normally degrade piperacillin. Tazobactam is derived from the penicillin nucleus and is a penicillinic acid sulfone.

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and 5050s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MM

Puromycin Dihydrochloride is an antibiotic. It inhibits protein synthesis by binding to RNA. Puromycin Dihydrochloride has antimicrobial, antitrypanosomal, and antineoplastic properties.

Puromycin is an aminoglycoside antibiotic isolated from the bacterium Streptomyces alboniger. It is a protein synthesis inhibitor.

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

Perhexiline maleate (WSM 3978G) is a prophylactic antianginal agent that inhibits carnitine palmitoyltransferase (CPT1/CPT2).

WP-1122(WP 1122) is a candidate drug to treat SARS-COV-2(COVID-19) .2-DG completely prevented SARS-CoV–2 replication in Caco–2 cells. Glycolysis is a process by which cells convert glucose into energy and infected (host) cells are induced by viruses to dramatically increase their dependence on glycolysis. WP1122 is a prodrug of 2-DG whereby chemical elements are added to 2-DG to improve its delivery in vivo.

Ghrelin agonist HM01 is a novel potent, orally available ghrelin (GHS-R) agonist with Ki of 1.42 nM (human GHS-R1a), induces potent activation of intracellular calcium signaling with EC50 of 1.25 nM.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

ML307 is a potent, sub-micromolar (IC50=781 nM), first-in-class, small molecule inhibitor of Ubc13 enzyme activity, >128-fold selective against Caspase-3 and Bfl-1.

RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively.

GLP-26 is a novel potent HBV capsid modulator that reduces secreted HBeAg in HepNTCPDL cells transfected with HBV wild type with EC50 of 0.7 uM.

ZHAWOC21026 is a highly potent, host-specific small-molecule inhibitor of paramyxovirus (Canine distemper virus, CDV IC50=3.2 nM) and pneumovirus (RSV, IC50=31 nM) replication.

RH-EDA is a rhodamine-based turn-on fluorescent probe for detecting hydroxyl radicals in living systems.

MS2734 is a bisubstrate Nicotinamide N-methyltransferase (NNMT) with IC50 of 14 uM, Kd of 2.7 uM..

EDA-DA is an unnatural dipeptide building block (an ethynyl-D-alanine and a D-alanine). It incorporates a biorthogonal alkyne group into peptidoglycan (PG) through MurF in the cytoplasmic pathway, which enables selective labeling via a click-chemistry reaction. EDA-DA allows labeling of PG in Gram-positive (B. subtilis), Gram-negative (E. coli and C. trachomatis), Mycobacterium (M. smegmatis) and moss plastids (P. patens) with azide modified fluorescent dyes such as Alexa Fluor 488.

Dalfopristin (RP54476) is a semi-synthetic analogue of ostreogyrcin A. Quinupristin/dalfopristin (Q/D) is a parental streptogramin with a spectrum of activity that includes Gram-positive pathogens, including those resistant to other classes of antimicrobial compounds.

LysoTracker Red (LysoTracker Red DND-99) is a paraformaldehyde fixable probe that concentrates into acidic compartments of cells and tissues. LysoTracker Red is an indicator of cell death in a manner similar to other standard assays (Annexin, terminal dUTP nick end labeling, Nile blue sulfate, neutral red, and acridine orange). LysoTracker Red is a marker for late endosomes and lysosomes.

Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.

MIN-101 (Roluperidone, CYR-101, MT-210) is a higly potent 5-HT2A and sigma 2 receptor antagonist, with no direct dopamine affinities, for treatment of negative symptoms in schizophrenia..

SRI-41315 is a small molecule that induces translational readthrough of CFTR nonsense mutations by eRF1 depletion, restores CFTR expression and function, suppresses CFTR nonsense mutations.SRI-41315 induces translational readthrough by depleting eRF1 protein level and prolonging the translational pause that occurs at premature termination codons (PTCs).SRI-41315 reduced eRF1 levels in a manner dependent upon a ubiquitin-mediated proteasome degradation pathway.SRI-41315 in combination with G418 restores CFTR function in primary bronchial epithelial cells derived from a CF patient with CFTR nonsense alleles.

MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells.