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SIS3 HCl
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SIS3 HCl图片
CAS NO:521984-48-5
包装与价格：
包装价格(元)
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SIS3HCl 是一种有效的选择性 Smad3 抑制剂，对 Smad3 磷酸化的 IC50 为 3 μM。
Cas No.521984-48-5
别名SIS3 盐酸盐
化学名(E)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one hydrochloride
Canonical SMILESCN1C(C2=CC=CC=C2)=C(C3=C1N=CC=C3)/C([H])=C([H])/C(N4CCC5=CC(OC)=C(OC)C=C5C4)=O.Cl
分子式C28H28ClN3O3
分子量489.99
溶解度≥ 49 mg/mL in DMSO, ≥ 11 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 3 μM

SIS3 HCI is an inhibitor of Smad3.

The receptor-associated Smads, such as Smad2 and Smad3, directly interact with activated TGF-receptor type I. Smads form heteromeric complexes with Smad4, which is a common mediator for all Smad pathways.

In vitro: In the reporter assay, it was found that the increased luciferase activity of p3TP-lux could be abrogated by the SIS3 HCI treatment in a dosedependent manner. Immunoprecipitation revealed SIS3 HCI attenuated the TGF-1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4. Whereas, SIS3 did not affect the phosphorylation of Smad2. In addition, it was found that SIS3 HCI attenuated the effects of TGF-1 by reducing the transcriptional activity. SIS3 HCI could also inhibit the myofibroblast differentiation of fibroblasts by TGF-1. Moreover, SIS3 HCI diminished the constitutive phosphorylation of Smad3 completely [1].

In vivo: Animal study showed that, in Tie2-Cre;Loxp-EGFP mice, AGEs could induce EndoMT. Immunoprecipitation and Western blotting showed that Smad3 could be activated by AGEs but was inhibited by SIS3 HCI in both MMECs and in STZ-induced diabetic nephropathy. Furthermore, confocal microscopy and real-time PCR showed that SIS3 HCI could abrogate EndoMT, reduce renal fibrosis, as well as retard nephropathy progression [2].

Clinical trial: Up to now, SIS3 HCI is still in the preclinical development stage.

References:
[1] Jinnin M et al. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression. Mol Pharmacol. 2006 Feb;69(2):597-607.
[2] Li J et al. Blockade of endothelial-mesenchymal transition by a Smad3 inhibitor delays the early development of streptozotocin-induced diabetic nephropathy. Diabetes.2010 Oct;59(10):2612-24.

 
 
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