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(E)-SIS3

Catalog No. T3636 CAS 521984-48-5

Synonyms: SIS3, SIS3 HCl

(E)-SIS3 (SIS3), a selective Smad3 inhibitor, can attenuate TGF-β1-dependent Smad3 phosphorylation and DNA binding. It has no effect on p38 MAPK, Smad2, ERK or PI3K signaling. It also inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts and inhibits TGF-β2-induced endothelial cell differentiation in iPSCs.

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(E)-SIS3, CAS 521984-48-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 176.00
25 mg	In stock	$ 363.00
50 mg	In stock	$ 538.00
100 mg	In stock	$ 768.00
500 mg	In stock	$ 1,550.00
1 mL * 10 mM (in DMSO)	In stock	$ 123.00

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Purity: 98.83%

Purity: 98%

Purity: 95.64%

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Storage & Solubility Information

Description	(E)-SIS3 (SIS3), a selective Smad3 inhibitor, can attenuate TGF-β1-dependent Smad3 phosphorylation and DNA binding. It has no effect on p38 MAPK, Smad2, ERK or PI3K signaling. It also inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts and inhibits TGF-β2-induced endothelial cell differentiation in iPSCs.
Targets&IC50	Smad3:3 µM.
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].
Cell Research	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.(Only for Reference)

Synonyms	SIS3, SIS3 HCl
Molecular Weight	489.99
Formula	C28H27N3O3·HCl
CAS No.	521984-48-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 23 mg/mL (46.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 90 mg/mL (183.7 mM)

References and Literature

1. Jinnin M, et al. Mol Pharmacol. 2006, 69(2):597-607. 2. Li J, et al. Diabetes. 2010, 59(10):2612-24.

Citations

1. Xu J, Ma L, Wang D, et al. Uncarboxylated osteocalcin promotes proliferation and metastasis of MDA-MB-231 cells through TGF-β/SMAD3 signaling pathway. BMC Molecular and Cell Biology. 2022, 23(1): 1-17

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library TGF-beta/Smad Compound Library Immunology/Inflammation Compound Library Covalent Inhibitor Library Cytokine Inhibitor Library Anti-Pancreatic Cancer Compound Library Reprogramming Compound Library Anti-Ovarian Cancer Compound Library Anti-Aging Compound Library

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Keywords

(E)-SIS3 521984-48-5 Stem Cells TGF-beta/Smad myofibroblast inhibit TGF-β1 SIS 3 SIS3 (E)SIS3 Smad3 Transforming growth factor beta fibroblasts differentiation (E) SIS3 phosphorylation (E)-SIS-3 SIS-3 SIS3 HCl Inhibitor inhibitor

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