Peptides for Drug Delivery

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.

DOTATATE is a DOTA-conjugated peptide. DOTATATE can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide research (PRRT). DOTATATE can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

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.

Unlabeled FXX489 (NNS309) is a ligand targeting fibroblast activation protein (FAP); its peptide component is the FAP-targeting peptide for FXX489 (HY-P10945). 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).

NOTA-FZCD-3 is a NOTA (HY-134418)-labeled FZCD-3 polypeptide precursor that targets cathepsin D (CTSD) with a K_D of 0.65 μM. NOTA-FZCD-3 binds specifically to the active site of CTSD, exhibits rapid in vivo clearance properties, and remains stable in blood for more than 2 h. NOTA-FZCD-3 can be used in studies monitoring CTSD-positive tumors.

RAD16-I, free acid TFA is a derivative of RADA16 (HY-P2632), with no Ac and NH2 modifications at both ends, and it has the same function as RADA16. RAD16-I, free acid TFA is a non-directed self-assembling peptide hydrogel. Under physiological conditions, RAD16-I, free acid TFA spontaneously forms a three-dimensional nanofiber network that mimics the extracellular matrix, and possesses excellent properties such as high water content, biocompatibility and degradability. RAD16-I, free acid TFA serves as an ideal scaffold for three-dimensional cell culture. RAD16-I, free acid TFA not only maintains cell viability and induces self-organization, but also supports cell adhesion, proliferation, differentiation and insulin secretion, effectively stabilizes islet clusters and promotes directed differentiation of the cardiac lineage. RAD16-I, free acid TFA can construct a cell-friendly nano-microenvironment for research related to diseases such as myocardial infarction and diabetes.

TAT-HA2 Fusion Peptide is a peptide-based delivery agent that combines the pH-sensitive HA2 fusion peptide from Influenza and the cell-penetrating peptide TAT from HIV. TAT-HA2 Fusion Peptide is a transactivator of transcription and hemaglutanin for endosomal release. TAT-HA2 Fusion Peptide enhances cellular uptake of macromolecules.

Angiopep-2-cys is a conjugate of Angiopep-2 hydrochloride (HY-P2341) and cysteine. 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.

DOTATATE acetate is a DOTA-conjugated peptide. DOTATATE acetate can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide research (PRRT). DOTATATE (acetate) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

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.

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.

Pentixafor is a peptide that targets CXCR4. Pentixafor is capable of being labelled with ⁶⁸Gallium (⁶⁸Ga) for positron emission tomography (PET) imaging. Pentixafor can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

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.

INF7 is a derivative of the N-terminal domain of the HA2 protein and is sensitive to pH. INF7 disrupts the stability of endosomal membranes through a mechanism independent of membrane fusion. INF7 can be used to enhance the endosome escape of complex or liposome-encapsulated proteins. Co-encapsulation of INF7 and molecular imaging probes in liposomes can enhance intracellular signaling and probe retention.

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

TAT (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus-1 (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins.

Peptide A5K (INF7-A5K-TAT) is an amphiphilic peptide derived from the HA2-TAT fusion scaffold. Peptide A5K can non-covalently bind to CRISPR ribonucleoproteins and efficiently deliver them to cells, such as primary human T cells, B cells, and NK cells. Peptide A5K enables low-toxicity, precise, and multiplex genome editing, holding great application potential in the field of cell therapy.

PSAR18-COOH (Ac-PSAR18-COOH) is a polysarcosine PSAR derivative. PSAR is a biodegradable, non-immunogenic polymer that has been used in a variety of compounds or diagnostic delivery systems. PSAR18 can be used as a component of ADC linkers.