activator

Nrf2 activator; inhibits Nrf2/Keap1 interaction. Induces upregulation of Nrf2 pathway downstream gene expression including heme-oxygenase 1. Suppresses LPS-induced TNF-α expression in THP-1 cells.

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.

Head activator neuropeptide, a mitogen for neuronal or neuroendocrine mammalian cell lines, induces mitosis by signaling through GPR37 binding [1].

The signal transducer and activator of transcription 6 fragments is a peptide with the sequence H2N-Ser-Tyr-Trp-Ser-Asp-Arg-Leu-Ile-Ile-OH, MW= 1152.3.

Colivelin is a neuroprotective peptide and activator of STAT3. Colivelin is a hybrid peptide synthesized to enhance the neuroprotective effects of humanin (HN).

740 Y-P acetate (740YPDGFR acetate) is a potent and cell-permeable PI3K activator.740 Y-P acetate tends to bind to GST fusion proteins containing the N- and C-terminal SH2 structural domains of p85, but not to GST alone.

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1 2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

740 Y-P(TFA) (740YPDGFR(TFA)) is a potent and cell-permeable activator of PI3K.

Angstrom6 (A-6 peptide) is an 8 amino acid peptide derived from single chain urokinase fibrinogen activator (scuPA) that interferes with the uPA uPAR cascade and abrogates the downstream effects.Angstrom6 has antitumor activity and inhibits tumor cell migration, invasion, and metastasis by binding to CD44 and modulating CD44-mediated cell signaling.

PKC fragment (530-558) is a peptide fragment of protein kinase C (PKC) and is a potent PKC activator. Protein Kinase C (530-558) significantly inhibits osteoclastic bone resorption.

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.

Guanylin (human) TFA is a 15-amino acid peptide that serves as an endogenous activator of intestinal guanylate cyclase. This compound is primarily located in the gastrointestinal tract, where it regulates electrolyte and water transport in the intestinal and renal epithelia through a mechanism dependent on cyclic GMP. [1][2]

LCKLSL, an N-terminal hexapeptide, acts as a competitive inhibitor of annexin A2 (AnxA2), effectively preventing the binding of tissue plasminogen activator (tPA) to AnxA2 while also inhibiting the generation of plasmin. In addition, LCKLSL exhibits anti-angiogenic properties.

4-Amino-L-phenylalanine (4APhe) is a TcCA activator, useful for studying protozoan pathogen infections.

ND1-YL2 is a peptide-based PROTAC®Degrader of steroid receptor co-activator 1 (SRC-1; also known as nuclear receptor coactivator 1, NCOA1). ND1-YL2 is composed of a stapled peptide that binds SRC-1 (YL2) joined by a linker to a tetrapeptide that binds UBR box domains. Upon ternary complex formation, SRC-1 is polyubiquitinated and subsequently degraded via the N-degron pathway. This Degrader induces dose-dependent degradation of SRC-1 in the MDA-MB-231 triple negative breast cancer cell line (DC50 = 10 μM), and binds to the PAS-B domain of SRC-1 (Ki = 320 nM). ND1-YL2 inhibits MDA-MB-231 cell migrationin vitro, and suppresses metastasis of MDA-MB-231 cellsin vivo.

TAME (Tosyl-Arginine Methyl Este), an inhibitor of the late-promoting complex (APC/C or APC), inhibits APC-dependent protein hydrolysis by competing for APC binding with the C-terminal isoleucine-arginine tail of the APC activator cytokinesis cycle 20 (Cdc20). TAME binds to and prevents APC binding by Cdc20 and Cdh20. TAME binds to APC and prevents its activation by Cdc20 and Cdh1.

Abaloparatide (BA 058), a parathyroid hormone receptor 1 (PTHR1) analog and selective activator, promotes Gs cAMP signaling and β-arrestin recruitment, thereby enhancing bone formation and improving cortical structure in mice. This compound holds potential for osteoporosis research [1] [2].

Dihexa (Hexanoyl-Tyr-Ile-Ahx-NH2) is an activator of the hepatocyte growth factor/c-Met (HGF/c-Met) system,it binds to HGF (Kd = 65 pM),and an analog of the peptide angiotensin IV.

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

CALP2 TFA, a potent calmodulin (CaM) antagonist with a dissociation constant (Kd) of 7.9 µM, exhibits high affinity for the CaM EF-hand Ca2+-binding site. This compound effectively inhibits CaM-dependent phosphodiesterase activity and elevates intracellular Ca2+ concentrations. Furthermore, it significantly hinders adhesion and degranulation, while also acting as a robust activator of alveolar macrophages [1] [2] [3] [4].

BAM(8-22) TFA, a proteolytically cleaved fragment of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), specifically MrgprC11 and hMrgprX1, inducing scratching in mice via an Mrgpr-dependent pathway [1].

TAT-14 TFA is a 14-mer peptide functioning as an Nrf2 activator possessing anti-inflammatory properties. It does not alter Nrf2 mRNA expression but elevates Nrf2 protein levels by targeting the Nrf2 binding site on Keap1 [1].

NFF-3 TFA, a selective matrix metalloproteinase (MMP) substrate, specifically interacts with MMP-3 and MMP-10 for hydrolysis. Additionally, it undergoes cleavage by trypsin, hepatocyte growth factor activator, and factor Xa. When labeled with the CyDye pair, Cy3 Cy5Q, NFF-3 TFA generates fluorescence in cell assays, facilitating the detection of cell activity [1].

Trichomide A, a natural cyclodepsipeptide, serves as a potent activator of SHP2. This compound exhibits immunosuppressive activity against activated T lymphocyte-mediated immune responses in Con A-activated T cells, highlighting its potential utility in researching immune-related skin diseases [1].