Peptide and Derivatives

DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR.

WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC₅₀ of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.

GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.

Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC₅₀ = 3 nM). Degarelix acetate Degarelix acetate (FE 200486) is used for the research of prostate cancer.

3X FLAG peptide TFA is a FLAG-tagged peptide containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide TFA can be used for protein separation and purification, and competitive elution with target proteins.

Zolucatetide (FOG-001;I-66) is a potent β-catenin inhibitor with an IC₅₀ of <50 nM. Zolucatetide can inhibits β-catenin and T-cell factor (TCF) transcription factor interaction. Zolucatetide inhibits cell proliferation and induces cell cycle arrest in target cells. Zolucatetide exhibits anti-tumor efficacy in mice bearing COLO320DM colon cancer cell (with APC, TP53 mutations) xenografts. Zolucatetide can be used for the study of colon cancer.

PACAP (1-38), human, ovine, rat is a PAC₁ receptor agonist. PACAP (1-38), human, ovine, rat binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC₅₀s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat increases the α-secretase activity. PACAP (1-38), human, ovine, rat elevates cytosolic Ca²⁺, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat can be used for neurotrophic and neuroprotective research.

Melittin is a PLA₂ activator, stimulates the activity of the low molecular weight PLA₂, while it does not the increase activity of the high molecular weight PLA₂.

Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Dulaglutide can be uesd for the research of type 2 diabetes (T2D) .

LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.

bFGF (119-126) is a ligand of bFGF. The complex formed by bFGF (119-126) and bFGF can bind to FGFR1, while inhibiting the bFGF-FGFR1 interaction, FGFR1 phosphorylation and downstream signaling pathways. Therefore, bFGF (119-126) induces cell apoptosis and inhibits cell proliferation, migration, angiogenesis and metastasis. When conjugated with a carrier, bFGF (119-126) enhances cellular uptake via FGFR-mediated endocytosis and serves as an effective FGFR-targeted ligand. When used in combination with ultrasound and Doxorubicin (HY-15142A), bFGF (119-126) significantly enhances the inhibitory effect on tumors. bFGF (119-126) is applicable to research related to lung cancer, breast cancer, glioblastoma and ovarian cancer.

PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC₅₀ of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

[Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer.

RGD is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.

Pegcetacoplan acetate is a pegylated complement C3/C3b inhibitor. Pegcetacoplan acetate acts by specifically binding to and inhibiting C3 and C3b, thereby suppressing the complement cascade at its proximal stage. Pegcetacoplan is not a known inhibitor or inducer of CYP450 isoenzymes. Pegcetacoplan acetate can be used for the research of complement-mediated diseases, including paroxysmal nocturnal hemoglobinuria (PNH) and age-related macular degeneration (AMD).

L-Carnosine is a dipeptide composed of beta-alanine and histidine. L-Carnosine is an endogenous metabolite found in human brain, muscle and gastrointestinal tissues and is present in all vertebrates. L-Carnosine is a non-enzymatic free radical scavenger and natural antioxidant with anti-inflammatory and neuroprotective properties that can inhibit biochemical changes associated with aging.

NFAT Inhibitor (VIVIT peptide) is an inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT.

Cardiotoxin Analog (CTX) IV (6-12) is a membrane active peptide that specifically targets negatively charged phospholipid membranes (such as phosphatidylserine and phosphatidylinositol). Cardiotoxin Analog (CTX) IV (6-12) was discovered in the venom of the Taiwan cobra. Cardiotoxin Analog (CTX) IV (6-12) is a chemically synthesized snake venom cardiotoxin that binds to cell membranes and embeds into lipid bilayers through hydrophobic interactions and electrostatic attraction, thereby destroying the stability of membrane structure. Cardiotoxin Analog (CTX) IV (6-12) can induce membrane lipid disorder and cell lysis, exhibiting hemolysis and cytotoxicity.

Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation.

OVA Peptide(257-264) TFA is a class I (Kb)-restricted peptide epitope of OVA, an octameric peptide can be from ovalbumin presented by the class I MHC molecule, H-2Kb.