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.

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.

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.

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.

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].

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.

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].

GP2-114 is a catecholamine motility mimetic that produces current-dependent cardiovascular effects when administered via transdermal iontophoresis and can be used to study coronary artery disease (CAD).

L-739750 2HCl is a potent inhibitor of peptidomimetic farnesyltransferase, a novel pseudopeptide mimetic with potential anticancer activity.

Itameline (RU 47213) can be used as a choline mimetic.

GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA).

Upacicalcet HCl is an intravesical calcium mimetic that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on calcium-sensitive receptors in parathyroid cell membranes, thereby lowering PTH levels in the blood.Upacicalcet HCl can be used for the treatment of blood Upacicalcet HCl is a novel compound for the treatment of secondary hyperparathyroidism, targeting amino acid-binding sites of calcium-sensitive receptors. binding sites.

PAOPA is a novel dopamine D2 receptor modulator and L-proline-L-leucine-glycine amide (PLG) peptide mimetic that prevents and reverses behavioral and biochemical abnormalities in preclinical animal models of schizophrenia sensitized to amphetamine. PAOPA has been used in the study of schizophrenia and extrapyramidal dysfunction.

GGTI-2133 is a potent mimetic peptidyl geranylgeranyltransferase type I inhibitor (GGTase I) with an IC50 value of 38 nM.GGTI-2133 inhibits the invasion of inflammatory cells into the airways in experimental asthma in mice.

Upacicalcet (AJT-240) is an intraventricular calcium mimetic, a SHPT available for human hemodialysis, that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on parathyroid cell membrane calcium-sensitive receptors, thereby lowering blood levels of PTH.Upacicalcet is an orthosteric modulator of calcium-sensitive receptors and prevents adenine-induced secondary vascular calcification and bone disease in a rat model of adenine-induced secondary hyperparathyroidism.

N-Acetylglycine is a minor constituent of food that is not genotoxic or acutely toxic and is capable of being used in biological studies of mimetic peptides.N-Acetylglycine acts as a blocker of the N-terminus of a peptide.3-Hydroxyanthranilic acid is a competitive succinate dehydrogenase inhibitor.

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

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.

Obatoclax (GX15-070), a pan-BCL-2 family proteins inhibitor and BH3 mimetic, exhibits a binding affinity (K_i) of 220 nM for BCL-2. It promotes autophagy-dependent cell death and cyclin D1 degradation via the proteasome. Additionally, Obatoclax demonstrates anti-cancer properties and broad-spectrum antiparasitic activity.

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.

Mito-TEMPO, a mitochondria-targeted superoxide dismutase mimetic, scavenges superoxide and alkyl radicals, preventing mitochondrial oxidation, necrosis, and apoptosis.

LCL161 is a SMAC mimetic, an IAP antagonist with oral activity that inhibits XIAP (IC50=35 nM) in HEK293 cells and also inhibits cIAP1 (IC50=0.4 nM) in MDA-MB-231 cells. LCL161 has potential antitumor activity.

Gap 26 is a mimetic peptide corresponding to the residues 63-75 of connexin 43, which is a gap junction blocker.

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.