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Domatinostat tosylate

Name: Domatinostat tosylate
Brand: TargetMol
SKU: T4477
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4477Cas No. 1186222-89-8

Alias 4SC-202

Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor targeting HDAC1/2/3 with IC50 values of 1.20/1.12/0.57 μM, respectively, and also inhibits Lysine-specific demethylase 1 (LSD1).

Domatinostat tosylate

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Purity: 97.35%

Catalog No. T4477Alias 4SC-202Cas No. 1186222-89-8

Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor targeting HDAC1/2/3 with IC50 values of 1.20/1.12/0.57 μM, respectively, and also inhibits Lysine-specific demethylase 1 (LSD1).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$35	In Stock	In Stock
5 mg	$81	In Stock	In Stock
10 mg	$123	In Stock	In Stock
25 mg	$228	In Stock	In Stock
50 mg	$372	In Stock	In Stock
100 mg	$558	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$109	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:97.35%

Appearance:Solid

Color:White

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COA HPLC LCMS HNMR

Product Introduction

Bioactivity

Description	Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor targeting HDAC1/2/3 with IC50 values of 1.20/1.12/0.57 μM, respectively, and also inhibits Lysine-specific demethylase 1 (LSD1).
Targets&IC50	HDAC11:9.7 μM, HDAC3:0.57 μM, HDAC10:21 μM, HDAC2:1.12 μM, HDAC1:1.2 μM, HDAC9:50 μM, HDAC5:11.3 μM
In vitro	Domatinostat provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat. Domatinostat-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat in HT-29 cells. Notably, Domatinostat, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. Domatinostat obviously reduces the proliferation of all epithelial and mesenchymal UC cell lines (IC50: 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity[1]. Domatinostat treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D[3].
In vivo	4SC-202 (i.g.) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2].
Synonyms	4SC-202

Chemical Properties

Molecular Weight	619.71
Formula	C₃₀H₂₉N₅O₆S₂
Cas No.	1186222-89-8
Smiles	Cc1ccc(cc1)S(O)(=O)=O.Cn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (80.68 mM), Sonication is recommended.

H2O: Insoluble

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.23 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6137 mL	8.0683 mL	16.1366 mL	80.6829 mL
5 mM	0.3227 mL	1.6137 mL	3.2273 mL	16.1366 mL
10 mM	0.1614 mL	0.8068 mL	1.6137 mL	8.0683 mL
20 mM	0.0807 mL	0.4034 mL	0.8068 mL	4.0341 mL
50 mM	0.0323 mL	0.1614 mL	0.3227 mL	1.6137 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