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SIS3 HCl

Cat. No. M8149
SIS3 HCl Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 70  USD70 In stock
5mg USD 110  USD110 In stock
10mg USD 200  USD200 In stock
25mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

SIS3 is a novel specific inhibitor of TGF-β1/ALK-5 phosphorylation of Smad3. SIS3 inhibits Smad3 phosphorylation with an IC50 of 3 µM. SIS3 inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.

SIS3 significantly reduces collagen IV and fibronectin expression in the glomeruli and tubulointerstitium of STZ-injected Tie2-Cre;Loxp-EGFP mice, suggesting that SIS3 retards the early development of STZ-induced diabetic glomerulosclerosis and tubulointerstitial fibrosis. However, SIS3 administration does not reduce proteinuria.

Chemical Information
Molecular Weight 489.99
Formula C28H27N3O3.HCl
CAS Number 521984-48-5
Solubility (25°C) DMSO: ≥ 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jinnin M, et al. Mol Pharmacol. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression.

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Keywords: SIS3 HCl supplier, TGF-beta/Smad, inhibitors, activators


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