PSB1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. It produces potent analgesic effects in vivo.

SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice.

Novel, potent and specific inhibitor of sphingosine kinase-1 (SphK1)

MRS1220 is a potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. MRS1220 displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors.

AGI-25696 (AGI 25696) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A, blocks the growth of MTAP-deleted tumors in vivo.

Neurokinin receptor antagonist with antiemetic activity

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).

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.

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.