KissPeptin-10

Kisspeptin-10 (KP-10; also known as Metastin 45-54) is a synthetic decapeptide corresponding to the C-terminal residues 112–121 of the KISS1 gene-encoded precursor protein (or residues 45–54 of metastin). It represents the minimal sequence of kisspeptin required for full activation of the kisspeptin receptor (KISS1R, previously known as GPR54 or AXOR12). The compound is a single, non-glycosylated polypeptide chain containing 10 amino acids and was first identified as the endogenous ligand for the orphan G protein-coupled receptor GPR54. Kisspeptin-10 has been extensively studied for its role in reproductive neuroendocrinology, particularly as a master regulator of the hypothalamic-pituitary-gonadal (HPG) axis through stimulation of gonadotropin-releasing hormone (GnRH) secretion. The compound is widely employed in research applications spanning reproductive biology, oncology, neuroendocrinology, and metabolic disorders.

Kisspeptin-10 exerts its effects by selectively binding to and activating the kisspeptin receptor KISS1R (GPR54), a class A G protein-coupled receptor (GPCR). Upon receptor activation, kisspeptin-10 triggers intracellular signaling cascades, including the activation of phospholipase C (PLC), mobilization of intracellular calcium, and phosphorylation of extracellular signal-regulated kinases (ERK1/2). The compound demonstrates high affinity for both rat and human KISS1 receptors, with Ki values of 1.59 nM and 2.33 nM, respectively. Activation of KISS1R in hypothalamic GnRH neurons stimulates the pulsatile secretion of GnRH, which in turn drives the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary. Beyond its canonical role in reproductive endocrinology, kisspeptin-10 has been shown to inhibit tumor metastasis and invasion, suppress angiogenesis through inhibition of VEGF expression and FAK/Rho GTPase activation, promote osteoblast differentiation via GPR54-mediated regulation of BMP2 expression, and exert neuroprotective effects.

• Reproductive Neuroendocrinology: Investigated as a master regulator of the HPG axis for studying GnRH secretion, LH/FSH release, puberty onset, and fertility regulation.
• Oncology and Metastasis Research: Employed to study tumor suppression mechanisms, inhibition of metastasis and invasion, and anti-angiogenic effects through suppression of VEGF expression.
• Bone and Osteoblast Differentiation: Studied for promoting osteogenic differentiation through GPR54-mediated NFATc4/BMP2 signaling, with applications in bone formation and regeneration research.
• Neuroprotection: Investigated for neurovascular protective effects following cerebral ischemia and preservation of blood-brain barrier integrity.
• Metabolic and Endocrine Disorders: Explored for therapeutic potential in gestational diabetes mellitus, polycystic ovary syndrome (PCOS), and infertility.
• Radiopharmaceutical Development: Utilized as a targeting vector for gallium-68/lutetium-177 labelled pan-tumour radiopharmaceuticals for cancer detection and therapy.

CAS Number: 374675-21-5 (human)
PubChem CID: 25240297
Molecular Formula: C₆₃H₈₃N₁₇O₁₄
Molecular Weight: 1,302.4–1,302.5 g/mol
Sequence: Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH₂ (YNWNSFGLRF-NH₂)
Purity: ≥ 99%
Form: Lyophilized powder
Storage: Store at ≤ -20°C in a cool, dry place, protected from light and moisture
Solubility: Soluble in sterile water (up to 1 mg/ml) and DMSO; prepare working solutions per laboratory protocol