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(E)-SIS3

Name: (E)-SIS3
Brand: TargetMol
SKU: T3636
Price: 36 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3636Cas No. 521984-48-5

Alias SIS3 hydrobromide, SIS3 HCl

(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) and is selective. (E)-SIS3 inhibits the differentiation of fibroblasts into myofibroblasts via TGF-β1.

(E)-SIS3

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Purity: 98%

Catalog No. T3636Alias SIS3 hydrobromide, SIS3 HClCas No. 521984-48-5

(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) and is selective. (E)-SIS3 inhibits the differentiation of fibroblasts into myofibroblasts via TGF-β1.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$36	In Stock	In Stock
2 mg	$52	In Stock	In Stock
5 mg	$113	In Stock	In Stock
10 mg	$176	In Stock	In Stock
25 mg	$363	In Stock	In Stock
50 mg	$538	In Stock	In Stock
100 mg	$768	In Stock	In Stock
500 mg	$1,550	-	In Stock
1 mL x 10 mM (in DMSO)	$123	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98%

Color:Yellow

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Product Introduction

Bioactivity

Description	(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) and is selective. (E)-SIS3 inhibits the differentiation of fibroblasts into myofibroblasts via TGF-β1.
Targets&IC50	Smad3:3 µM.
In vitro	METHODS: Human dermal fibroblasts were treated with (E)-SIS3 (10 μM) for 24 hours, and the expression levels of target proteins were detected by Western Blot and Immunoprecipitation. RESULTS: (E)-SIS3 attenuated TGF-beta1-induced Smad3 phosphorylation and Smad3 / Smad4 interaction. [1] METHODS: Human dermal fibroblasts were treated with (E)-SIS3 (0.1-50 μM) for 30 minutes, and the expression levels of target proteins were detected by Western Blot. RESULTS: (E)-SIS3 significantly inhibited the expression of FN and α-SMA, but not the expression of Sphk2 induced by TGF-β1. [2] METHODS: Human dermal fibroblasts were treated with (E)-SIS3 (10 μM) for 24 hours, and the expression levels of target proteins were detected by Western Blot. RESULTS: (E)-SIS3 significantly decreased the expression of α-SMA and Palladin in primary human dermal fibroblasts. [3]
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 hydrobromide, SIS3 HCl

Chemical Properties

Molecular Weight	489.99
Formula	C₂₈H₂₇N₃O₃·HCl
Cas No.	521984-48-5
Smiles	Cl.COc1cc2CCN(Cc2cc1OC)C(=O)\C=C\c1c(-c2ccccc2)n(C)c2ncccc12
Relative Density.	no data available

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 23 mg/mL (46.94 mM), Sonication is recommended.

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

DMSO: 100 mg/mL (204.09 mM), Sonication and heating are recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.73 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0409 mL	10.2043 mL	20.4086 mL	102.0429 mL
5 mM	0.4082 mL	2.0409 mL	4.0817 mL	20.4086 mL
10 mM	0.2041 mL	1.0204 mL	2.0409 mL	10.2043 mL
20 mM	0.1020 mL	0.5102 mL	1.0204 mL	5.1021 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0408 mL	0.2041 mL	0.4082 mL	2.0409 mL
100 mM	0.0204 mL	0.1020 mL	0.2041 mL	1.0204 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc