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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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 489.99
Formula C28H27N3O3.HCl
CAS Number 521984-48-5
Purity 99.53%
Solubility DMSO: ≥ 70 mg/mL
Storage at -20°C
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

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