Exploring kartogenin: advances in therapeutics and signaling mechanisms for musculoskeletal regeneration

Kartogenin (KGN) is a small synthetic heterocyclic molecule with chondrogenic and chondroprotective effects. Since its discovery, there has been a focus on regenerating cartilage damage and treating Osteoarthritis) OA(. In the treatment of OA, it’s important to target both cartilage and subchondral...

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Bibliographic Details
Published in:Molecular biology reports Vol. 52; no. 1; p. 533
Main Authors: Kiani, Sareh, Fallahi, Jafar, Tanideh, Nader, Razban, Vahid, Khajeh, Sahar
Format: Journal Article
Language:English
Published: Dordrecht Springer Netherlands 01.12.2025
Springer Nature B.V
Subjects:
aesthetics
ambient temperature
Anilides - pharmacology
Anilides - therapeutic use
Animal Anatomy
Animal Biochemistry
Animals
Biomedical and Life Sciences
Bone growth
Bone healing
Bone Regeneration - drug effects
Cancellous bone
Cartilage
Cartilage diseases
Cell differentiation
Cell Differentiation - drug effects
Cell signaling
Chondrocytes
Chondrocytes - drug effects
Chondrocytes - metabolism
Chondrogenesis
Chondrogenesis - drug effects
Clinical trials
drugs
heterocyclic compounds
Histology
Humans
inflammation
Life Sciences
ligands
Morphology
musculoskeletal system
Osteoarthritis
Osteoarthritis - drug therapy
Osteoarthritis - metabolism
pain
Phthalic Acids - pharmacology
Phthalic Acids - therapeutic use
Regeneration
Regeneration - drug effects
Review
Signal Transduction - drug effects
Sox9 protein
SOX9 Transcription Factor - metabolism
Subchondral bone
therapeutics
Toxicity
Wound healing
Wound Healing - drug effects
Kartogenin
Regeneration
Signaling
SOX9
Chondrogenesis
ISSN:0301-4851, 1573-4978, 1573-4978
Online Access:Get full text
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Summary:Kartogenin (KGN) is a small synthetic heterocyclic molecule with chondrogenic and chondroprotective effects. Since its discovery, there has been a focus on regenerating cartilage damage and treating Osteoarthritis) OA(. In the treatment of OA, it’s important to target both cartilage and subchondral bone. KGN appears to reduce cartilage degradation and changes in subchondral trabecular bone. It can also reduce inflammation and pain behavior in vitro and in vivo. Additionally, KGN promotes chondrocyte differentiation and proliferation. It has been applied in many regenerative research fields including aesthetic procedures, limb skeletal growth, wound healing, tendon and bone regeneration and disc regeneration. KGN is similar to the natural ligands involved in cell signaling and differentiation. The master regulator of cartilage genes, Sex‑determining region‑box 9 protein (SOX9), is upregulated by KGN, making it an ideal drug to promote cartilage repair. Advantages of KGN include demonstrated low toxicity across various cell types and no apparent adverse effects in animals. It is highly stable, easily stored at room temperature, and can be synthesized inexpensively and efficiently. Analogues of KGN have entered clinical trials.
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ISSN:0301-4851
1573-4978
1573-4978
DOI:10.1007/s11033-025-10653-6