SIS3 HCl

製品コードS7959 バッチS795903

印刷

化学情報

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

49 mg/mL (100.0 mM)

Ethanol

3 mg/mL (6.12 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.45mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 49 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.3mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

参考

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：

UBR5 mediates colorectal cancer chemoresistance by attenuating ferroptosis via Lys 11 ubiquitin-dependent stabilization of Smad3-SLC7A11 signaling [ Redox Biol, 2024, 76:103349]	PubMed: 39260061
Vulnerability to APOBEC3G linked to the pathogenicity of deltaretroviruses [ Proc Natl Acad Sci U S A, 2024, 121(13):e2309925121]	PubMed: 38502701
Vulnerability to APOBEC3G linked to the pathogenicity of deltaretroviruses [ Proc Natl Acad Sci U S A, 2024, 121(13):e2309925121]	PubMed: 38502701
Therapeutic targeting of PLK1 in TERT promoter-mutant hepatocellular carcinoma [ Clin Transl Med, 2024, 14(5):e1703]	PubMed: 38769666
Therapeutic targeting of PLK1 in TERT promoter-mutant hepatocellular carcinoma [ Clin Transl Med, 2024, 14(5):e1703]	PubMed: 38769666
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
SETD2 deficiency promotes renal fibrosis through the TGF-β/Smad signalling pathway in the absence of VHL [ Clin Transl Med, 2023, 13(11):e1468]	PubMed: 37933774

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。