Toremifene Citrate(NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.

ITX-5061 is a scavenger receptor B1 antagonist that promotes high-density lipoprotein (HDL) levels.

UKH-1114 (UKH1114) is a potent, sigma 2 receptor/Tmem97 agonist with Ki of 46 nM.

NACE2i is a cell permeable, specific and selective peptide inhibitor of nuclear ACE2, inhibits binding between IMP1α and ACE2 and SARS-CoV-2 viral replication. NACE2i specifically targets nuclear ACE2 and not other nuclear proteins targeted by the importin pathway. NACE2i has no impact on ACE2 enzymatic activity. NACE2i prevents inflammation and macrophage infiltration, and increases NK cell infiltration in bronchioles. NACE2i treatment increases the levels of the active histone mark, H3K27ac, restores host translation in infected hamster bronchiolar cells, and leads to an enrichment in methylated ACE2 in hamster bronchioles and lung macrophages. NACE2i has a dual mode of action: suppressing the lethal inflammation in severe COVID-19 and inhibiting viral replication by restoring host translation of anti-viral cytokines.

Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A.

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

BRD 7389 is an inhibitor of ribosomal S6 kinases (RSK) with IC50 of 1.5 uM, 2.4 uM, and 1.2 uM for RSK1, RSK2, and RSK3, respectively.

CPT is a potent adenosine A1 receptor antagonist.

Brassinin is a Inducer of phase II enzymes. Moderate and competitive indoleamine 2,3-dioxygenase inhibitor (Ki = 98 μM). Shows chemopreventive effects in vivo. Orally active.

SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria.

A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.

LUN76721 has CAS#4376-72-1, is a cyclophosphazene and a useful chemical reagent. Cyclophosphazenes have been studied among others as flame retardant additives, high temperature fluids, clathrates, photostabilizers, or antioxidants in organic polymers. Cyclophosphazenes have also been used as phase transfer catalysts, as polypodants and cryptands. Cyclophosphazenes have also been successfully used as biologically active agents. Moreover cyclotriphosphazenes, were used for polymer functionalization and synthesis, as pendant groups or monomers for polyphosphazene synthesis, especially those bearing six chlorine atoms or phenoxy groups.

Metipranolol is a non-selective beta blocker used in eye drops to treat glaucoma. It is rapidly metabolized into desacetylmetipranolol.

GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 also is a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.

TC-DAPK 6 is an oxazalone compound that acts as a potent, ATP-competitive, and highly selective death-associated protein kinase (DAPK) inhibitor (IC50 = 69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 uM ATP).

MINA53 inhibitor (Compound 10) is a first-in-class inhibitor of the ribosomal oxygenase MINA53 with an IC50 of 1.5 μM in vitro.

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.

AXC-715 trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715 trihydrochloride, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.

PSB603 is a adenosine A(2B) receptor antagonist which suppresses tumor growth and metastasis by inhibiting induction of regulatory T cells.

Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.

ZHAWOC9045 (F2205-0189) is a potent, host-specific small-molecule inhibitor of paramyxovirus (Canine distemper virus, CDV IC50=0.7 uM) and pneumovirus (RSV, IC50=5.9 uM) replication.ZHAWOC9045 displays broad-spectrum antiviral activity, inhibits CDV in a host cell-dependent manner.

Prinomastat (AG3340) is a potent, selective MMP inhibitor with pM affinities for inhibiting gelatinases (MMP-2 and -9, Ki=50-150 pM), MMP-14 and MMP-13; demonstrates broad antitumor activity in a number of tumor models, inhibits glioma invasion or growth of the human malignant glioma cell line U87; also suppresses tumor growth in a malignant glioma tumor model.

Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.

QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5

A potent, orally bioavailable dual CXCR2/CXCR1 receptor antagonist with IC50 of 1.3 nM and 7.3 nM, respectively.

Gramicidin is a combination of six different antimicrobial polypeptides (from Bacillus aneurinolyticus (Bacillus brevis)).

VKGILS-NH2 serves as the reversed amino acid sequence control peptide for SLIGKV-NH2, a protease-activated receptor 2 (PAR2) agonist.