For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Kartogenin(KGN) is a small molecule stimulator of chondrogenesis; promotes chondrocyte differentiation(EC50=100 nM) and binds to filamin A.<br>IC50 value: 100 nM(EC50, promotes chondrocyte differentiation) [1]<br>Target: Chondrogenesis stimulator<br>Kartogenin is a small molecule kartogenin, which promotes chondrocyte differentiation (median effective concentration = 100 nM), shows chondroprotective effects in vitro, and is efficacious in two OA animal models. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program [1]. KGN stimulated type-I collagen synthesis of fibroblasts at the mRNA and protein levels in a time-dependent manner, but KGN did not induce expression of α-skeletal muscle actin (α-sma) or matrix metallopeptidase1 (MMP1), MMP9 in vitro [2]. KGN promoted the type-I collagen synthesis of dermal fibroblasts in vitro and in the dermis of mice through activation of the smad4/smad5 pathway.<br>in vivo: KGN also increased type-I collagen synthesis in the dermis of BALB/C mice [2].</p>
Catalog Number | I003636 |
CAS Number | 4727-31-5 |
Synonyms | 2-[(4-phenylphenyl)carbamoyl]benzoic acid |
Molecular Formula | C20H15NO3 |
Purity | ≥95% |
Target | Wnt/β-catenin |
Solubility | DMSO: ≥ 42 mg/mL |
Storage | Store at +4C |
IC50 | 100 nM(EC50, promotes chondrocyte differentiation) [1] |
InChI | InChI=1S/C20H15NO3/c22-19(17-8-4-5-9-18(17)20(23)24)21-16-12-10-15(11-13-16)14-6-2-1-3-7-14/h1-13H,(H,21,22)(H,23,24) |
InChIKey | SLUINPGXGFUMLL-UHFFFAOYSA-N |
SMILES | OC(C1=CC=CC=C1C(NC2=CC=C(C3=CC=CC=C3)C=C2)=O)=O |
Reference | </br>1:The combined use of kartogenin and platelet-rich plasma promotes fibrocartilage formation in the wounded rat Achilles tendon entheses. Zhang J, Yuan T, Zheng N, Zhou Y, Hogan MV, Wang JH.Bone Joint Res. 2017 Apr;6(4):231-244. doi: 10.1302/2046-3758.64.BJR-2017-0268.R1. PMID: 28450316 Free PMC Article</br>2:Hyaluronic Acid Hydrogel Functionalized with Self-Assembled Micelles of Amphiphilic PEGylated Kartogenin for the Treatment of Osteoarthritis. Kang ML, Jeong SY, Im GI.Tissue Eng Part A. 2017 Mar 24. doi: 10.1089/ten.tea.2016.0524. [Epub ahead of print] PMID: 28338415 </br>3:Development of kartogenin-conjugated chitosan-hyaluronic acid hydrogel for nucleus pulposus regeneration. Zhu Y, Tan J, Zhu H, Lin G, Yin F, Wang L, Song K, Wang Y, Zhou G, Yi W.Biomater Sci. 2017 Mar 28;5(4):784-791. doi: 10.1039/c7bm00001d. PMID: 28261733 </br>4:Kartogenin with PRP promotes the formation of fibrocartilage zone in the tendon-bone interface. Zhou Y, Zhang J, Yang J, Narava M, Zhao G, Yuan T, Wu H, Zheng N, Hogan MV, Wang JH.J Tissue Eng Regen Med. 2017 Jan 27. doi: 10.1002/term.2258. [Epub ahead of print] PMID: 28127950 </br>5:Modulation of Superficial Zone Protein/Lubricin/PRG4 by Kartogenin and Transforming Growth Factor-β1 in Surface Zone Chondrocytes in Bovine Articular Cartilage. Miyatake K, Iwasa K, McNary SM, Peng G, Reddi AH.Cartilage. 2016 Oct;7(4):388-97. doi: 10.1177/1947603516630789. Epub 2016 Feb 22. PMID: 27688846 Free PMC Article</br>6:Kartogenin treatment prevented joint degeneration in a rodent model of osteoarthritis: A pilot study. Mohan G, Magnitsky S, Melkus G, Subburaj K, Kazakia G, Burghardt AJ, Dang A, Lane NE, Majumdar S.J Orthop Res. 2016 Oct;34(10):1780-1789. doi: 10.1002/jor.23197. Epub 2016 Mar 1. PMID: 26895619 </br>7:Creating an Animal Model of Tendinopathy by Inducing Chondrogenic Differentiation with Kartogenin. Yuan T, Zhang J, Zhao G, Zhou Y, Zhang CQ, Wang JH.PLoS One. 2016 Feb 5;11(2):e0148557. doi: 10.1371/journal.pone.0148557. eCollection 2016. PMID: 26848746 Free PMC Article</br>8:Kartogenin-Incorporated Thermogel Supports Stem Cells for Significant Cartilage Regeneration. Li X, Ding J, Zhang Z, Yang M, Yu J, Wang J, Chang F, Chen X.ACS Appl Mater Interfaces. 2016 Mar 2;8(8):5148-59. doi: 10.1021/acsami.5b12212. Epub 2016 Feb 16. PMID: 26844837 </br>9:Photo-Cross-Linked Scaffold with Kartogenin-Encapsulated Nanoparticles for Cartilage Regeneration. Shi D, Xu X, Ye Y, Song K, Cheng Y, Di J, Hu Q, Li J, Ju H, Jiang Q, Gu Z.ACS Nano. 2016 Jan 26;10(1):1292-9. doi: 10.1021/acsnano.5b06663. Epub 2016 Jan 12. PMID: 26757419 </br>10:Kartogenin, transforming growth factor-β1 and bone morphogenetic protein-7 coordinately enhance lubricin accumulation in bone-derived mesenchymal stem cells. Liu C, Ma X, Li T, Zhang Q.Cell Biol Int. 2015 Sep;39(9):1026-35. doi: 10.1002/cbin.10476. Epub 2015 May 7. PMID: 25857705 |