activating

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

Proteasome-activating peptide 1 TFA is a potent activator of the proteasome, enhancing chymotrypsin-like proteasomal catalytic activity and increasing proteolytic rates both in vitro and in culture. It also inhibits protein aggregation in cellular models of amyotrophic lateral sclerosis (ALS) [1].

Proteasome-activating peptide 1 enhances chymotrypsin-like proteasomal catalytic activity, boosting proteolytic rates both in vitro and within cultured cells. Additionally, it inhibits protein aggregation in a cellular model of amyotrophic lateral sclerosis [1].

PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate) is an agonist of Protease-Activated Receptor-2 (PAR-2).

Sperm-activating peptide 1 is a bioactive chemical.

Macrophage-activating lipopeptide 2 TFA (MALP-2 TFA) is a diacylglycerol lipopeptide and TLR-2/TLR-6 agonist that activates immune cell responses such as macrophages, upregulating TNF, IL-6, and PGE2 to induce local inflammation.

Rusalatide acetate (TP508 amide acetate), a regenerative peptide, mitigates radiation-induced gastrointestinal injury by activating stem cells and preserving mucosal integrity.

Octapeptide-2 Acetate, as a hair growth promotion active, is a double-layered encapsulated biomimetic peptide that helps increase cell growth and migration. It promotes hair growth by activating the stem cells of the hair follicles. Octapeptide-2 is more stable and prolongs action than native proteins.

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in normal human pancreas and adrenal gland tissue and in some tumors that produce vasoactive intestinal peptide (VIP). PRP (1-29) is secreted by CHO-K1 cells that express human recombinant preproPACAP.

Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml). Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).

TLQP-21 TFA, a VGF-derived peptide with endocrine and extraendocrine properties, acts as a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM), activating C3aR1 to increase intracellular Ca2+ levels, and is used in research on nociception regulation and other relevant physiological functions[1][2].

[Lys8, Lys9]-Neurotensin (8-13) (JMV438) is a Neurotensin analog that elicits analgesic effects by activating the G protein-coupled receptors NTS1 and NTS2, with K i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.

KRAS G13D peptide, a 25-mer sequence, is derived from the KRAS activating oncogene mutation and serves as an immune potentiator. This peptide possesses immunogenic properties and can be utilized for the development of a KRAS vaccine.

EPQpYEEIPIYL, a phosphopeptide, is a ligand for the Src homology 2 (SH2) domain, activating Src family members such as Lck, Hck, and Fyn through binding interactions with SH2 domains.

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist with an EC50 of 10.9 nM for kappa opioid receptor activation, used in peripheral pain research.

Cyclo(his-pro) is an endogenous cyclic dipeptide that exerts oxidative damage protection by selectively activating the transcription factor Nrf2 signalling pathway.

TAT peptide (TFA), a cell-penetrating peptide (GRKKRRQRRRPQ) originating from HIV-1's trans-activating transcriptional activator (Tat), facilitates intracellular delivery [1] [2].

MMK1 TFA is a potent, selective agonist for the human formyl peptide receptor like-1 (FPRL-1 FPR2), exhibiting EC50 values of <2 nM for FPRL-1 and >10,000 nM for FPR1. This compound acts as a powerful chemotactic and calcium-mobilizing agent, effectively activating phagocytic leukocytes. It significantly enhances the Pertussis Toxin-sensitive production of proinflammatory cytokines IL-1b and IL-6 by human monocytes. Additionally, MMK1 TFA has been demonstrated to exhibit anxiolytic-like activity [1] [2] [3] [4].

Ac9-25 TFA, an N-terminal peptide of Annexin I, functions as a formyl peptide receptor (FPR) agonist, activating neutrophil NADPH oxidase via FPR [1] [2].

Lys-γ3-MSH(human) TFA, a melanocortin peptide originating from the C-terminal fragment of pro-opiomelanocortin (POMC), enhances the steroidogenic response of rat adrenal glands to adrenocorticotrophin (ACTH). It is a potent stimulator of lipolysis, demonstrating an apparent EC50 of 3.56 nM, by activating hormone-sensitive lipase (HSL) and Perilipin A, leading to lipolysis [1] [2].