mimetic

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

EUK-134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities and inhibits the formation of β-amyloid and related amyloid fibrils.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

NBD-556 is a small molecule mimetic of CD4. NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.

Xevinapant hydrochloride (AT-406 HCl) , an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide.

Manganese(salen) chloride (EUK-8) is a superoxide dismutase and catalase mimetic, serving as an antioxidant with oxyradical scavenging properties, and ameliorates acute lung injury in endotoxemic swine.

Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

Xevinapant (Debio-1143) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.

SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a "closed" activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.

Indoximod (NLG-8189) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.

EPO Mimetic Peptide-1 (EMP-1) is a 20 amino acid peptide that promotes cell proliferation, modulates the cell cycle, and stimulates reticulocyte production in vivo [1].

Connexin mimetic peptide 40GAP27, corresponding to the GAP27 domain of the second extracellular loop of the dominant vascular connexin (Cx40), designated as 40Gap27, is a biologically active peptide utilized to study the pathways by which oxidant stress hinders gap junction communication. Administered 40Gap27 attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.

Connexin mimetic peptide 40,37GAP26, a biologically active peptide, matches the GAP26 domain of the extracellular loop of major vascular connexins Cx37 and Cx40, referred to as 37,40Gap26 based on Cx homology. It has been utilized to examine gap junctions' involvement in propagating endothelial hyperpolarizations induced by cyclopiazonic acid (CPA) in the rodent iliac artery wall. Abundant gap junction plaques comprising Cx37 and Cx40 are present in the endothelium, and the peptide exerts inhibitory actions on subintimal hyperpolarization.

The ApoA-I mimetic peptide (PVLDLFRELLNELLEALKQKLK) exhibits potent activation of lecithin:cholesterol acyl transferase (LCAT). It is also utilized in the synthesis of peptide/lipid complexes [1] [2].

Apo A-I mimetic 5A peptide is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). It facilitates the efflux of cholesterol from inside cells, helping to reduce intracellular cholesterol accumulation. Additionally, Apo A-I mimetic 5A peptide exhibits anti-inflammatory properties, lowering inflammatory markers in blood and tissues. This peptide is used in cardiovascular disease research.

NH-3 is a potent orally active thyroid hormone receptor (THR) antagonist which exhibits reversible behavior, demonstrated by an IC 50 of 55 nM. Derived from the selective thyromi-metic GC-1, NH-3 effectively inhibits the binding of thyroid hormones to their respective receptors, resulting in hindered cofactor recruitment.

Pancuronium dibromide (Pavulon), a competitive AChR antagonist (IC50 = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide(Pancuronium bromide) blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.

Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.

Cefsulodin sodium (Sulcephalosporin) hydrate is a β lactam antibiotic.

Synephrine (Oxedrine) is sympathetic alpha-adrenergic agonist used as a vasoconstrictor in circulatory failure, asthma, nasal congestion, and glaucoma.

Rivastigmine tartrate (SDZ-ENA 713) is a carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE.

Bethanechol chloride (Carbamyl-β-methylcholine chloride) is a slowly hydrolyzing muscarinic agonist with no nicotinic effects. It is used to increase smooth muscle tone in the GI tract following abdominal surgery or to treat urinary retention without obstruction. Possible side effects include hypotension, heart rate changes, and bronchial spasm.

Synephrine hydrochloride (Oxedrine hydrochloride) is an agonist that acts on sympathomimetic α-adrenergic receptor (AR).