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My CartCAS：521984-48-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 521984-48-5 |
| Name | (E)-SIS3 |
| Molecular Formula | C28H27N3O3HCl |
| Molecular Weight | 489.99 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD09265258 |
| SMILES | CN1C2=NC=CC=C2C(/C=C/C(N3CCC(C=C(OC)C(OC)=C4)=C4C3)=O)=C1C5=CC=CC=C5.[H]Cl |
| Target Point | Smad3 |
| Passage | TGF-beta/Smad;Stem Cells |
| Background | SIS3 is a novel specific Smad3 inhibitor. |
| Biological Activity | (E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1[1]. |
| IC50 | 3μM(Smad3 phosphorylation)[1] |
| In Vitro | (E)-SIS3(0.3-10 μM; for 1 hour)attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1].(E)-SIS3(0.1 ，10，50 μM; 30 min)significantly suppresses the expression of FN and α-SMA，but not that of Sphk2 provoked by TGF-β1[2].(E)-SIS3(10 μM; 24 hours)significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts[3].(E)-SIS3 significantly inhibits L4 development at five concentrations from as low as 2 μM to 50 μM(5 μM，10 μM，20 μM and 50 μM)in a dose-dependent manner[4]. |
| Data Literature Source | [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]. Zhu X，et al. Sphingosine kinase 2 cooperating with Fyn promotes kidney fibroblast activation and fibrosis via STAT3 and AKT. Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [3]. Liu J，et al. Topical TWEAK Accelerates Healing of Experimental 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. |
| Unit | Piece |
| Specification | 5mg 10mM*1mL in DMSO 10mg 25mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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