Peptide Profile
GHK-Cu
Copper-Binding Tripeptide / Metallopeptide
CLINICAL DEVELOPMENT STAGE:
Phase 2
GHK-Cu is a naturally occurring copper-binding tripeptide complex studied for its effects on extracellular matrix remodeling, collagen and glycosaminoglycan synthesis, dermal fibroblast activity, tissue repair, and wound-healing pathways.
Compound Overview
Molecular Formula
C₁₄H₂₂N₆O₄·Cu
Molecular Weight
401.91 g/mol
CAS Number
89030-95-5
Classification
Copper-Binding Tripeptide / Metallopeptide
Regulatory Status
Investigational; not FDA approved
Targets / Receptors
Copper(II) binding and transport; extracellular matrix signaling; MMP-2 regulation; TIMP-1 and TIMP-2 regulation; collagen synthesis pathways; glycosaminoglycan synthesis; fibroblast activity; antioxidant and inflammatory signaling
Research Focus
Copper transport and binding; extracellular matrix remodeling; collagen synthesis; glycosaminoglycan synthesis; dermal fibroblast activity; tissue repair; wound-healing signaling; antioxidant and inflammatory pathway regulation
Mechanism of Action
GHK-Cu is formed when the naturally occurring tripeptide glycyl-L-histidyl-L-lysine binds a copper(II) ion. Unlike peptides that act primarily through a defined cell-surface receptor, GHK-Cu does not have a single established canonical receptor.
Its biological activity appears to involve copper transport and modulation of multiple cellular pathways associated with extracellular matrix production, collagen synthesis, tissue remodeling, fibroblast activity, and cellular repair.
Experimental studies have also shown effects on matrix metalloproteinases and their tissue inhibitors, suggesting a role in coordinated extracellular matrix remodeling.
Research Evidence
Much of the mechanistic evidence for GHK-Cu comes from cell and animal research, including studies showing effects on fibroblast activity, glycosaminoglycan synthesis, collagen-related pathways, and extracellular matrix remodeling.
Human evidence is more limited and has produced mixed results. Small controlled studies have evaluated copper-tripeptide formulations in skin repair and wound-related settings, but these studies have not consistently demonstrated significant objective improvements.
Clinical development is continuing. A Phase 2 clinical trial initiated in 2026 is evaluating topical GHK-Cu for acute skin wound healing, including re-epithelialization, wound-area reduction, scar quality, and safety. Results have not yet been reported.
Safety & Limitations
GHK-Cu has substantial laboratory and preclinical literature, but controlled human evidence remains comparatively limited. Findings from cultured cells and animal wound models cannot be assumed to establish the same effects in humans.
Existing human studies have produced mixed findings, and the current Phase 2 wound-healing study has not yet reported results. GHK-Cu is not FDA approved as a therapeutic drug, and its long-term safety, systemic pharmacology, and efficacy for proposed therapeutic applications have not been established through large controlled clinical trials.
Key References
- Freedman JH, et al. Structure of the glycyl-L-histidyl-L-lysine-copper(II) complex in solution. Biochemistry. 1982.
- Wegrowski Y, et al. Stimulation of sulfated glycosaminoglycan synthesis by the tripeptide-copper complex glycyl-L-histidyl-L-lysine-Cu²⁺. Life Sciences. 1992.
- Siméon A, et al. The tripeptide-copper complex GHK-Cu stimulates matrix metalloproteinase-2 expression by fibroblast cultures. Life Sciences. 2000.
- Miller DM, et al. Effects of topical copper tripeptide complex on CO₂ laser-resurfaced skin. Archives of Facial Plastic Surgery. 2006.
- Topical GHK-Cu Gel for Acute Skin Wound Healing. ClinicalTrials.gov. Phase 2 clinical trial.
Last scientifically reviewed: August 27, 2026
