Targeting Peptides

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors.

Cyclic somatostatin (SRIF-14) is a growth hormone-release inhibiting factor used in the research of severe, acute hemorrhages of gastroduodenal ulcers. Cyclic somatostatin is a neuropeptide co-stored with acetylcholine in the cardiac parasympathetic innervation, exerts influences directly on contraction of ventricular cardiomyocytes. Cyclic somatostatin inhibits the contractile response of isoprenaline with an IC₅₀ value of 13 nM. Cyclic somatostatin can be used for the research of cardiovascular disease.

iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.

RP-182 acetate is a synthetic immunomodulatory peptide that exerts anti-tumor effects by targeting the mannose receptor CD206 (K_d = 8 μM) on the surface of tumor-associated macrophages (TAMs). RP-182 acetate induces a conformational switch of the CD206 receptor, which activates NF-κB signaling and phagocytosis in CD206^high TAMs. RP-182 acetate has dual function: activation of canonical NF-κB signaling, triggering TNFα secretion and autocrine activation of the TNF receptor 1 (TNFR1), leading to activation of caspase 8, apoptosis, and cell death. RP-182 acetate is used in pancreatic cancer and melanoma research.

Osteocalcin (Osteocalcin (1-49)) (human) TFA is a vitamin K-dependent bone specific protein. Osteocalcin (human) TFA is chemotactic for several of the cell types frequently found at bone remodeling surfaces.

CTP (cardiac targeting peptide) can transduce cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be reversibly linked (e.g. via enolases, thiol groups) to cargo (e.g. miRNAs) for delivery specifically to cardiomyocytes over all other organs.

Angiopep-2 hydrochloride is a brain peptide vector. The conjugation of anticancer agents with the Angiopep-2 peptide vector could increase their efficacy in the treatment of brain cancer.

Cyclo(RGDyK) is a potent and selective α_Vβ₃ integrin inhibitor with an IC₅₀ of 20 nM.

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the α_vβ₃ integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

Cyclo[Arg-Gly-Asp-D-Phe-Lys(Azide)] is the derivative of Cyclo(-RGDfK) (HY-P0023). Cyclo[Arg-Gly-Asp-D-Phe-Lys(Azide)] is a click chemistry reagent containing an azide group. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity.

WYRGRL is a selective, high-affinity collagen type II-binding peptide with a IC₅₀ of 140 nM. Collagen type II is the most abundant and specific structural protein in the extracellular matrix of articular cartilage. WYRGRL can precisely target small-molecule compounds such as Dexamethasone (HY-14648) and nanocarrier-engineered exosomes to cartilage, significantly enhancing their therapeutic effects on osteoarthritis.

HAIYPRH hydrochloride, a targeting ligand, can specially bind to transferrin receptor (TfR). HAIYPRH hydrochloride can mediate the transport of nanocarriers across the blood-brain barrier.

Muscle homing peptide M12 can preferentially bind to surface protein of muscle cells. Muscle homing peptide M12 mediates enhanced cellular uptake of nanoparticles (NPs) in myoblasts in vitro. Muscle homing peptide M12 is covalently conjugated to PLGA-PEG NPs via the N-terminal α-amino groups of peptides using the N-hydroxysuccinimide ester reaction.

CSTSMLKAC (peptide 2) is a cyclic 9 amino acid sequence that mimics endogenous peptide sequences. CSTSMLKAC homes to cardiomyocytes in the ischemic myocardium.

Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with ⁶⁸Ga and ¹⁷⁷Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC).

Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors.

GPC3 targeting peptide 1 TFA is a GPC3 targeting peptide, with a K_d value of 0.23 nM.