Caprooyl tetrapeptide-3 (Caprooyl-Gly-His-Lys-Lys) is a potent growth factor mimetic, widely utilized in cosmetic products for anti-wrinkle, firming, post-surgical repair, and stretch mark prevention.
It stands as one of the rare DEJ (Dermal-Epidermal Junction)-targeting peptides within the current anti-aging arsenal that combines high activity, exceptional stability, and low irritation.
This peptide is developed through the simulation and optimization of GHK, a wound-healing fragment derived from Transforming Growth Factor. While natural GHK upregulates the synthesis and activation of Collagen VII, Laminin-5, and Fibronectin, its clinical application is limited by a short plasma half-life and poor skin retention.
The unique N-terminal ε-amino hexanoic acid acylation in caprooyl tetrapeptide-3 enhances its compatibility with human stratum corneum lipids by 6-fold, significantly boosts key protein expression, increases skin permeability by 4-fold, and markedly improves biological signal transduction, thereby overcoming the inherent limitations of natural GHK as a topical active.
The biomimetic, naturally reparative mechanism of caprooyl tetrapeptide-3 has led to its widespread adoption in high-end cosmetics and has significantly accelerated progress in wrinkle improvement research.1
Sequence
Caprooyl-Gly-His-Lys-Lys
CAS Number
1012317-71-3
Molecular Formula
C32H59N9O11
Molecular Weight
745.86
Caprooyl Tetrapeptide-3 Related Research
1.Core Mechanisms and Multidimensional Efficacy
Furthermore, its distinctive biomimetic structure enables multi-targeted, synergistic anti-aging and cosmetic benefits. It retains the core activity of the endogenous GHK-Cu peptide, stimulating the synthesis and assembly of Type I, III, and IV collagen as well as fibronectin, while concurrently inhibiting the overexpression of matrix metalloproteinases.
This leads to a significant improvement in skin condition and promotes a lasting youthful appearance. Additionally, it upregulates the synthesis of basement membrane zone proteins, strengthening DEJ stability and enhancing overall skin firmness and tolerance.
2.Promotion of Collagen Synthesis Function
Caprooyl tetrapeptide-3 retains the core sequence of the endogenous GHK peptide, allowing it to efficiently chelate copper ions (Cu²⁺) and form active complexes in the body.
This, in turn, upregulates the transcriptional activity of collagen-related genes within cells, stimulating the synthesis of Type I and Type III collagen.
It can significantly increase collagen density and thickness in the dermis, improving skin density and reducing fine lines and wrinkles caused by collagen loss.
In clinical practice, long-term use of caprooyl tetrapeptide-3 has been shown to visibly improve static wrinkles such as nasolabial folds and crow’s feet.2
3.Inhibition of Excessive Matrix Metalloproteinase Activation
Caprooyl tetrapeptide-3 suppresses the overactivation of matrix metalloproteinases triggered by stressors such as UV exposure.
At the genetic level, it interferes with normal signal transduction pathways, downregulating the synthesis and activation of interstitial collagenase and gelatinase.
This provides maximal protection for the integrity and stability of the existing skin extracellular matrix structure, thereby extending the period of youthful skin appearance and markedly retarding the skin aging process in mature individuals. 3
4.Strengthening of Dermal-Epidermal Cell Connections and Barrier Function
Caprooyl tetrapeptide-3 upregulates the synthesis and activation of Type IV collagen, laminin, and Type XVII collagen.
This reinforces the dermal-epidermal junction, enhances nutrient exchange efficiency between dermal and epidermal cells, and promotes tighter intercellular connections.
Consequently, it improves the skin’s intrinsic supportive structure, resulting in a fuller, more resilient texture.
Overall, it enhances the skin barrier function, reduces moisture loss, and improves skin tolerance.
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