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Chemical Structure| 530141-72-1 Chemical Structure| 530141-72-1

Structure of T-5224
CAS No.: 530141-72-1

Chemical Structure| 530141-72-1

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T-5224 is a selective c-Fos/JunD heterodimer inhibitor with an IC50 value of 5 μM for AP-1. T-5224 exhibits anti-inflammatory and antitumor effects and can be used in research on inflammatory diseases and cancer.

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Product Details of T-5224

CAS No. :530141-72-1
Formula : C29H27NO8
M.W : 517.53
SMILES Code : O=C(O)CCC1=CC(C(C2=CC=C(OC3CCCC3)C=C2O)=O)=CC=C1OCC4=CC=C5C(NOC5=C4)=O
MDL No. :MFCD28053483
InChI Key :DALCQQSLNPLQFZ-UHFFFAOYSA-N
Pubchem ID :23626877

Safety of T-5224

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

Isoform Comparison

Biological Activity

Description
T-5224 serves as an inhibitor of the transcription factor c-Fos/activator protein (AP)-1, offering anti-inflammatory benefits by specifically targeting the DNA binding activity of c-Fos/c-Jun, while leaving other transcription factors unaffected. It effectively prevents the IL-1β-induced increase in the transcription of Mmp-3, Mmp-13, and Adamts-5[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
RPTEC/TERT1 OAT3 cells 50 µM 4 hours To study the effect of T-5224 on TGFB1 expression, results showed that T-5224 significantly decreased TGFB1 expression. PMC6949151
Rat aorta smooth muscle cells (RASMCs) 10 µM 24 hours T-5224 inhibited AP-1 activity, leading to a significant downregulation of c-KIT expression in RASMCs and restoring the F-actin changes induced by M2Es. PMC7482821
FTC133 cells 10 μM 40 hours To test the effect of T-5224 on GABPB promoter activity, results showed that T-5224 inhibited GABPB promoter activity. PMC7980366
Various thyroid cancer cells 10 μM To test the effect of T-5224 on cancer cell viability, results showed that mutant TERT cells were more sensitive to T-5224. PMC7980366

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice DRO and SK-MEL-3 xenograft tumor models Oral 30 mM Continuous consumption To test the effect of T-5224 on tumor growth, results showed that T-5224 significantly suppressed the growth of mutant TERT tumors. PMC7980366

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.66mL

1.93mL

0.97mL

19.32mL

3.86mL

1.93mL

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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