SIS3 HCl

製品コードS7959 バッチS795901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H27N3O3.HCl
分子量 489.99 CAS No. 521984-48-5
Solubility (25°C)* 体外 DMSO 97 mg/mL (197.96 mM)
Ethanol 24 mg/mL (48.98 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
in vitro Addition of SIS3 attenuates the effects of TGF-β1 by reducing the transcriptional activity. SIS3 also inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 completely diminishes the constitutive phosphorylation of Smad3 as well as the up-regulated type I collagen expression in scleroderma fibroblasts, thus abolishes the ECM overexpression in the TGF-β1-treated normal dermal fibroblasts and scleroderma fibroblasts in vitro[1].
in vivo SIS3 inhibits Smad3 activation in streptozotocin(STZ)-induced diabetic nephropathy in Tie2-Cre;Loxp-EGFP mice. It also reduces AGE-induced EndoMT and decreases EndoMT in STZ-induced diabetic nephropathy in Tie2-Cre;Loxp-EGFP mice. 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[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Normal human dermal fibroblasts, Scleroderma fibroblasts
濃度 0.3, 1, 3 μM
反応時間 72 h
実験の流れ

Normal human dermal fibroblasts are plated at a density of 105 cells/well in six-well culture plates and grown until subconfluence in MEM containing 10% FCS. Cells are quiesced by 24-h incubation in serum-free MEM, followed by incubation in serum-free medium in the presence or absence of SIS3 before the collection of cells for 72 h. Then, the cells are detached from the wells by trypsin treatment and counted using a Coulter counter.
動物実験 動物モデル Male C57BL/6J mice
投薬量 1, 2.5, or 5 μg/g
投与方法 i.p.

カスタマーフィードバック

, , Circ Res, 2017, 121(6):617-627

Data from [Data independently produced by , , Cell Physiol Biochem, 2017, 44(6):2201-2211]

Data from [Data independently produced by , , Lab Invest, 2018, doi: 10.1038/s41374-018-0091-y]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Treatment for type 2 diabetes and diabetic nephropathy by targeting Smad3 signaling [ Int J Biol Sci, 2024, 20(1):200-217] PubMed: 38164169
Sleeve gastrectomy links the attenuation of diabetic kidney disease to the inhibition of renal tubular ferroptosis through down-regulating TGF-β1/Smad3 signaling pathway [ J Endocrinol Invest, 2024, 10.1007/s40618-023-02267-1] PubMed: 38512446
Smad3 is essential for polarization of tumor-associated neutrophils in non-small cell lung carcinoma [ Nat Commun, 2023, 14(1):1794] PubMed: 37002229
Smad3 is essential for polarization of tumor-associated neutrophils in non-small cell lung carcinoma [ Nature Communications-, 2023, 1794-2023)] PubMed: None
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546] PubMed: 37428012
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546] PubMed: 37428012
Suppression of TGFβR-Smad3 pathway alleviates the syrinx induced by syringomyelia [ Cell Biosci, 2023, 13(1):98] PubMed: 37248485
Smad3 Mediates Diabetic Dyslipidemia and Fatty Liver in db/db Mice by Targeting PPARδ [ Int J Mol Sci, 2023, 24(14)11396] PubMed: 37511155
Investigating the Role of TGF-β Signaling Pathways in Human Corneal Endothelial Cell Primary Culture [ Cells, 2023, 12(12)1624] PubMed: 37371094
Resveratrol inhibits TGF-β1-induced fibrotic effects in human pterygium fibroblasts [ Environ Health Prev Med, 2023, 28:59] PubMed: 37866886

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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