SIS3 盐酸盐作用机制 - Medchemexpress - MCE中国

1、Product Data Sheet(E)-SIS3Cat. No.: HY-13013CAS No.: 521984-48-5分式: CHClNO分量: 489.99作靶点: TGF-beta/Smad作通路: Stem Cell/Wnt; TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (61.23 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 m

2、g 10 mgConcentration制备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验 请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 I

3、n Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天 使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可 以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.10 mM); Clear solution此案可获得 2.5 mg/mL (5.10 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L

4、 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 (E)-SIS3种有效和选择性的 Smad3 抑制剂，抑制 Smad3 磷酸化的 IC50 为 3 M。(E)-SIS3 通过 TGF-1 抑制成纤维细胞向肌成纤维细胞分化。IC & Target IC50: 3 M (Smad3 phosphorylation)1体外研究 (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.户使本产品发表的科研献 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