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.

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

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.

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.

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).

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

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

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.

Compstatinis is a 13-residue cyclic peptide, and a potent inhibitor of the complement system.

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740 Y-P is a peptide activator of phosphatidylinositol 3-kinase (PI3K).

PAR2 receptor agonist

Agonist peptide derived from the N-terminus of protease-activated receptor-2 (PAR2). Activates PAR2 (EC50 ~ 5 μM) and facilitates gastrointestinal transit in mice in vivo.

Inhibitor of furin (Ki values are 0.106, 0.58 and 13.2 μM for furin, PACE4 and PC1 respectively).

Diprotin A is a tripeptide inhibitor of dipeptidyl peptidase 4

Teglicar, in vitro and in animal models, reduces gluconeogenesis and improves glucose homeostasis, refreshing the interest in selective and reversible L-CPT1 inhibition as a potential antihyperglycemic approach.

Daporinad, also known as APO-866 and FK866, is a small molecule with potential antineoplastic and antiangiogenic activities. NMPRTase inhibitor APO866 binds to and inhibits nicotinamide phosphoribosyltransferase (NMPRTase), inhibiting the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell prioduction of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis.

CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.

Tamibarotene(Am-80) is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.

Mirk-IN-1 is a potent, specific inhibitor of Dyrk1B (Mirk kianse) and Dyrk1A with IC50 of 68 nM and 22 nM respectively, shows SW620 cell IC50 of 1.9 uM.

INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.

EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.

EN460 is a specific mall molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1), interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation (IC50=1.9 uM).