SIS3 鹽酸鹽作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data Sheet(E)-SIS3Cat. No.: HY-13013CAS No.: 521984-48-5分式: CHClNO分量: 489.99作靶點(diǎn): TGF-beta/Smad作通路: Stem Cell/Wnt; TGF-beta/Smad儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30 mg/mL (61.23 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 m

2、g 10 mgConcentration制備儲(chǔ)備液1 mM 2.0409 mL 10.2043 mL 20.4086 mL5 mM 0.4082 mL 2.0409 mL 4.0817 mL10 mM 0.2041 mL 1.0204 mL 2.0409 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 I

3、n Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.10 mM); Clear solution此案可獲得 2.5 mg/mL (5.10 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L

4、 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 (E)-SIS3種有效和選擇性的 Smad3 抑制劑，抑制 Smad3 磷酸化的 IC50 為 3 M。(E)-SIS3 通過 TGF-1 抑制成纖維細(xì)胞向肌成纖維細(xì)胞分化。IC & Target IC50: 3 M (Smad3 phosphorylation)1體外研究 (E)-SIS3 (0.3-10 M; f

5、or 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction ofSmad3 with Smad41.(E)-SIS3 (0.1, 10, 50M; 30min) significantly suppresses the expression of FN and -SMA, but not that of Sphk2provoked by TGF-12.(E)-SIS3 (10 M; 24 hours) significantly reduces both -SMA and pallad

6、in expression that is enhanced by TWEAK inPrimary human dermal fibroblasts3.(E)-SIS3 significantly inhibits L4 development at five concentrations from as low as 2 M to 50 M (5 M, 10 M, 20M and 50 M) in a dose-dependent manner4.Western Blot Analysis1Cell Line: Human dermal fibroblastsConcentration: 0

7、.3, 1, 3, 10 MIncubation Time: For 1 hourResult: Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction ofSmad3 with Smad4.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Invest Dermatol. 2019 Jan;139(1):224-234. J Cell Physiol. 2019 Jun 23. Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. Sci Rep.

8、 2017 Sep 8;7(1):11006. Front Pharmacol. 2018 Jun 21;9:660.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Jinnin M et al. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellularmatrix ex

9、pression. Mol Pharmacol. 2006 Feb;69(2):597-607.2. Zhu X, et al. Sphingosine kinase 2 cooperating with Fyn promotes kidney fibroblast activation and fibrosis via STAT3 and AKT. Biochim Biophys Acta MolBasis Dis. 2018 Nov;1864(11):3824-3836.3. Liu J, et al. Topical TWEAK Accelerates Healing of Experi

10、mental Burn Wounds in Mice. Front Pharmacol. 2018 Jun 21;9:660.4. Li FF, et al. Identification and characterization of an R-Smad homologue (Hco-DAF-8) from Haemonchuscontortus. Parasit Vectors. 2020 Apr 3;13(1):164.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been fully validated for medical appli