Kartogenin
(Synonyms: 2-([1,1-联苯]-4-基氨基甲酰)苯甲酸,KGN) 目录号 : GC15057
Kartogenin是软骨样组织形成的诱导剂(EC50: 100 nM)。
Cas No.:4727-31-5
Sample solution is provided at 25 µL, 10mM.
Kartogenin is an inducer of cartilage-like tissue formation (EC50: 100nM) [1]. Kartogenin activates chondrogenesis and promotes cartilage matrix synthesis by regulating signaling pathways such as filaminA/CBFβ/RUNX1, Ihh, and TGF-β/Smad [2-3]. Kartogenin is commonly used to treat osteoarthritis and tendon repair [4].
In rabbit bone marrow stromal cells (BMSCs), Kartogenin (1nM–5µM; 3d) enhances cell proliferation and induces chondrogenic differentiation of stem cells in a concentration-dependent manner [5]. In rat cartilage-derived chondrogenic stem/progenitor cells (CSPCs), Kartogenin (10µM; 7d) promotes the proliferation of cell [6].
In surgically induced osteoarthritis mouse model, Kartogenin (1μM, 100μM; intra-articular injection; 4 weeks) prevents cartilage degradation and alleviates osteoarthritis progression in mice via the miR-146a/NRF2 axis [7]. In monoiodoacetate-induced osteoarthritis mouse model, Kartogenin (100μM; intra-articular injection; 14d) inhibits pain behavior, chondrocyte inflammation, and attenuates osteoarthritis progression in mice through induction of IL-10 [8].
References:
[1]. Johnson K A. A stem cell-based approach to cartilage repair[J]. Osteoarthritis and Cartilage, 2013, 21: S4.
[2]. Cai J, Zhang L, Chen J, et al. Kartogenin and its application in regenerative medicine[J]. Current medical science, 2019, 39(1): 16-20.
[3]. Bhuyan S, Swain S, Misra R D K, et al. Nanomedicine-Driven Approaches for Kartogenin Delivery: Advancing Chondrogenic Differentiation and Cartilage Regeneration in Tissue Engineering[J]. International Journal of Nanomedicine, 2025: 7443-7468.
[4]. Im G I. Application of kartogenin for musculoskeletal regeneration[J]. Journal of Biomedical Materials Research Part A, 2018, 106(4): 1141-1148.
[5]. Zhang J, Wang J H C. Kartogenin induces cartilage-like tissue formation in tendon–bone junction[J]. Bone research, 2014, 2(1): 1-10.
[6]. Liu T, Li X, Wang T, et al. Kartogenin mediates cartilage regeneration by stimulating the IL-6/Stat3-dependent proliferation of cartilage stem/progenitor cells[J]. Biochemical and Biophysical Research Communications, 2020, 532(3): 385-392.
[7]. Hou M, Zhang Y, Zhou X, et al. Kartogenin prevents cartilage degradation and alleviates osteoarthritis progression in mice via the miR-146a/NRF2 axis[J]. Cell death & disease, 2021, 12(5): 483.
[8]. Kwon J Y, Lee S H, Na H S, et al. Kartogenin inhibits pain behavior, chondrocyte inflammation, and attenuates osteoarthritis progression in mice through induction of IL-10[J]. Scientific reports, 2018, 8(1): 13832.
Kartogenin是软骨样组织形成的诱导剂(EC50: 100 nM) [1]。Kartogenin通过调节细丝蛋白A/CBFβ/RUNX1、Ihh和TGF-β/Smad等信号通路来激活软骨形成并促进软骨基质合成 [2-3]。Kartogenin常用于治疗骨关节炎和肌腱修复 [4]。
在兔骨髓基质细胞(BMSCs)中,Kartogenin(1nM-5µM;3d)以浓度依赖性方式增强细胞增殖并诱导干细胞向软骨形成分化 [5]。在大鼠软骨来源的软骨形成干细胞/祖细胞(CSPCs)中,Kartogenin(10µM;7d)促进细胞增殖 [6]。
在手术诱发的骨关节炎小鼠模型中,Kartogenin(1μM,100μM;关节内注射;4周)通过miR-146a/NRF2轴防止小鼠软骨退化并减轻骨关节炎进展 [7]。在单碘乙酸诱发的骨关节炎小鼠模型中,Kartogenin(100μM;关节内注射;14d)通过诱导IL-10抑制小鼠疼痛行为、软骨细胞炎症并减缓骨关节炎进展 [8]。
Cell experiment [1]: | |
Cell lines | Rabbit bone marrow stromal cells (BMSCs) |
Preparation Method | Rabbit BMSCs were seeded in 6-well plates at a density of 6×104 per well and cultured for two weeks in growth medium with various concentrations (1nM–5µM) of Kartogenin. The medium was changed every 3 days and after 2 weeks, cell proliferation was measured by population doubling time (PDT), and cell differentiation was assessed by measuring the expression of chondrogenic markers (aggrecan, collagen type II and Sox-9) using quantitative RT-PCR (qRT-PCR), cytochemical and immunocytochemical staining for proteoglycans, collagen type II and osteocalcin. |
Reaction Conditions | 1nM–5µM; 3d |
Applications | Kartogenin enhances cell proliferation and induces chondrogenic differentiation of stem cells in a concentration-dependent manner. |
Animal experiment [2]: | |
Animal models | Surgically induced osteoarthritis mouse model |
Preparation Method | A knee osteoarthritis (OA) model was established in six- to eight-week-old male C57BL/6J mice using DMM (medial meniscus instability transection) surgery. Mice were anesthetized with 2% isoflurane in 30% oxygen, and the medial meniscotibial ligament was transected using microscissors by the same surgeon. A sham surgery group was treated with joint capsule exposure but no ligamentous integrity was altered. Following surgery, intra-articular injections of 10μL of saline were administered to the control group, while 1μM or 100μM Kartogenin solutions (Kartogenin dissolved in DMSO and diluted in 0.9% saline) were administered to the experimental groups twice weekly. MiR-146a mimics were used simultaneously in some mice to further explore its protective effect on Kartogenin. |
Dosage form | 1μM, 100μM; intra-articular injection; 4 weeks |
Applications | Kartogenin prevents cartilage degradation and alleviates osteoarthritis progression in mice via the miR-146a/NRF2 axis. |
References: |
Cas No. | 4727-31-5 | SDF | |
别名 | 2-([1,1-联苯]-4-基氨基甲酰)苯甲酸,KGN | ||
化学名 | 2-[(4-phenylphenyl)carbamoyl]benzoic acid | ||
Canonical SMILES | O=C(C1=CC=CC=C1C(O)=O)NC2=CC=C(C=C2)C3=CC=CC=C3 | ||
分子式 | C20H15NO3 | 分子量 | 317.34 |
溶解度 | ≥ 10.6mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 3.1512 mL | 15.756 mL | 31.5119 mL |
5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL |
10 mM | 0.3151 mL | 1.5756 mL | 3.1512 mL |
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