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Chemical Structure| 521984-48-5 Chemical Structure| 521984-48-5

Structure of SIS3 HCl
CAS No.: 521984-48-5

Chemical Structure| 521984-48-5

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(E)-SIS3 is a potent and selective Smad3 inhibitor with an IC50 of 3 μM for Smad3 phosphorylation. It inhibits the myofibroblast differentiation of fibroblasts induced by TGF-β1.

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Product Details of SIS3 HCl

CAS No. :521984-48-5
Formula : C28H28ClN3O3
M.W : 489.99
SMILES Code : O=C(N1CC2=C(C=C(OC)C(OC)=C2)CC1)/C=C/C3=C(C4=CC=CC=C4)N(C)C5=NC=CC=C53.[H]Cl
MDL No. :MFCD09265258
InChI Key :CDKIEBFIMCSCBB-CALJPSDSSA-N
Pubchem ID :16079005

Safety of SIS3 HCl

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
Primary hepatocytes 10 μM 6 hours Pretreatment with SIS3 attenuated TGF-β-induced Lpcat2/4 and Smpd3 gene expression PMC3077083
bone marrow-derived NK cells 2 µM 3 hours To investigate the inhibitory effect of SIS3 on TGF-β1-mediated E4BP4 mRNA expression PMC5343519
spleen-derived NK cells 2 µM 3 hours To investigate the inhibitory effect of SIS3 on TGF-β1-mediated E4BP4 mRNA expression PMC5343519
HK-2 human proximal tubular epithelial cells 5 µM 30 hours Treatment with SIS3 significantly suppressed cadmium-induced HK-2 cell death PMC6889492
MPC5 cells 5 μM 24 hours SIS3 inhibited TGF-β1-induced Btg2 expression and Smad3 signaling, thereby preventing EMT and fibrotic phenotype in MPC5 cells. PMC10646233

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice B16F10 or LLC tumour models intraperitoneal (i.p.) 20 mg/kg Once daily for 17 consecutive weeks To investigate the inhibitory effect of SIS3 on tumour growth, results showed that SIS3 significantly suppressed tumour growth and increased NK cell production PMC5343519
Mice Rlbp1-GFP mice Intraperitoneal injection 50 mg/kg Honokiol, 1 mg/mouse Cetuximab once every two days for 16 days To investigate the effect of SIS3 on the retinal injury response in mice, it was found that SIS3 treatment significantly reduced the formation of glial scars and promoted the dedifferentiation of Müller cells. PMC8482586

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.20mL

2.04mL

1.02mL

20.41mL

4.08mL

2.04mL

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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