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Chemical Structure| 4727-31-5 Chemical Structure| 4727-31-5

Structure of Kartogenin
CAS No.: 4727-31-5

Chemical Structure| 4727-31-5

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Kartogenin can activate the smad4/smad5 pathway and promote the differentiation of multipotent mesenchymal stem cells into chondrocytes.

Synonyms: KGN

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Product Details of Kartogenin

CAS No. :4727-31-5
Formula : C20H15NO3
M.W : 317.34
SMILES Code : O=C(O)C1=CC=CC=C1C(NC2=CC=C(C3=CC=CC=C3)C=C2)=O
Synonyms :
KGN
MDL No. :MFCD00560510
InChI Key :SLUINPGXGFUMLL-UHFFFAOYSA-N
Pubchem ID :2826191

Safety of Kartogenin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Rabbit patellar tendon stem/progenitor cells 1 nM - 5 μM 2 weeks KGN enhanced cell proliferation in a concentration-dependent manner and induced chondrogenic differentiation of stem cells, as demonstrated by high expression levels of chondrogenic markers aggrecan, collagen II and Sox-9. Additionally, KGN induced the formation of cartilage-like tissues in cell cultures, as observed through the staining of abundant proteoglycans, collagen II and osteocalcin. PMC4237211
Rabbit bone marrow stromal cells 1 nM - 5 μM 2 weeks KGN enhanced cell proliferation in a concentration-dependent manner and induced chondrogenic differentiation of stem cells, as demonstrated by high expression levels of chondrogenic markers aggrecan, collagen II and Sox-9. Additionally, KGN induced the formation of cartilage-like tissues in cell cultures, as observed through the staining of abundant proteoglycans, collagen II and osteocalcin. PMC4237211
Human umbilical cord mesenchymal stem cells (UC-MSC) 10 μM 24 h To detect the cleavage products of KGN in UC-MSC, 4-ABP and PA were found, and 4-ABP was stronger than KGN in promoting chondrogenic differentiation. PMC6831301
Rat bone marrow mesenchymal stem cells (BMSC) 10 μM 3 days To evaluate the effects of KGN, 4-ABP, and PA on chondrogenic differentiation of BMSC, 4-ABP significantly promoted chondrogenic differentiation, while PA did not. PMC6831301
Chondrocytes 0.01 μM, 0.1 μM, 1 μM 1, 3, 5, 7 days KGN significantly enhanced the synthesis of cartilage matrix components such as type II collagen and aggrecan, and markedly suppressed the expression of matrix-degradation enzymes such as MMP13 and ADAMTS5. PMC8119954
Mesenchymal stem cells (MSCs) 100 nM 72 h To investigate the effect of KGN-MNPs on chondrogenic differentiation of MSCs, the results showed that KGN significantly upregulated the gene expression of type II collagen, aggrecan, and lubricin. PMC9696621
Chondrocytes 100 nM 24 and 48 h Evaluate the pro-inflammatory activity of PN-KGN nanospheres, results showed that PN-KGN had no pro-inflammatory effects on chondrocytes. PMC6058480
Chondrocytes 0, 10, 100 nM 4 or 7 days Evaluate the cytotoxicity of PN-KGN nanospheres on cell viability, results showed that PN-KGN had no cytotoxicity in chondrocytes. PMC6058480
Rat nucleus pulposus cells 0.01, 0.1, 1 μM KGN promoted ECM synthesis in NPCs under normal culture conditions and inhibited catabolic activities in IL-1β-stimulated NPCs, involving the activation of NRF2 and downstream antioxidant enzymes PMC10407629
Human nucleus pulposus cells (hNPCs) 100 nmol/ml and 1 µmol/ml 24 and 48 h To explore whether Kartogenin can slow down the degeneration of nucleus pulposus cells induced by IL-1β and TNF-α. The results showed that Kartogenin significantly elevated the expression of type II collagen and aggrecan in hNPCs. PMC5752177

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Rat patellar tendon model and rat Achilles tendon-bone junction injury model Injection 100 μM(10 μL) Injected on days 1, 2, 7, and 14, lasting for 15 days KGN induced cartilage-like tissue formation in the injected area. In the Achilles tendon-bone junction injury model, KGN enhanced wound healing, as evidenced by the formation of extensive cartilage-like tissues. PMC4237211
Mice Destabilization of medial meniscus (DMM)-induced osteoarthritis model Oral 5 mg/kg Daily for one month To evaluate the protective effects of oral KGN administration in a DMM-induced osteoarthritis model, KGN significantly improved cartilage injury, and only 4-ABP was detected in cartilage. PMC6831301
Mice Post-traumatic OA model Intra-articular injection 1 μM, 100 μM Twice a week for four weeks KGN ameliorated cartilage degeneration and inhibited subchondral bone sclerosis. PMC8119954
Sprague-Dawley rats Anterior cruciate ligament transection (ACLT) model Intra-articular injection 100 nM Once a week for 7 weeks To investigate the therapeutic effect of KGN-MNPs in the ACLT model, the results showed that KGN-MNPs significantly improved cartilage degeneration, reduced subchondral bone changes, and extended the injection interval. PMC9696621
SD rats Osteoarthritis model Intra-articular injection 100 µM Every 3 weeks for 9 weeks Evaluate the therapeutic effects of PN-KGN in the OA model, results showed that the PN-KGN injection group had significantly less cartilage degeneration at 12 weeks, indicating that PN-KGN could further arrest the development of OA. PMC6058480
Rats Puncture-induced intervertebral disc degeneration model Injection 25 mg/mL 4 and 8 weeks post-surgery KGN-enhanced dynamic hydrogel ameliorated puncture-induced intervertebral disc degeneration by restoring local redox homeostasis PMC10407629
Mice Intervertebral disc organ culture model Added to culture medium 100 nM/ml and 1 µM/ml 3 and 10 days To explore whether Kartogenin can slow down the degeneration of intervertebral discs induced by IL-1β and TNF-α. The results showed that Kartogenin significantly elevated the expression of type II collagen and aggrecan in mouse intervertebral discs. PMC5752177

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.76mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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