Art. -Nr.: HY-16012A

Domatinostat

(Synonyms: 4SC-202 free base)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC₅₀ of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).

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Reinheit: 99.34%
CAS. Nr.: 910462-43-0
Formel: C₂₃H₂₁N₅O₃S
Molecular Weight:447.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Domatinostat Chemical Structure

CAS. Nr.: 910462-43-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[4]

HDAC-3

0.57 μM (IC₅₀)

HDAC-2

1.12 μM (IC₅₀)

HDAC-1

1.2 μM (IC₅₀)

HDAC-11

9.7 μM (IC₅₀)

HDAC-5

11.3 μM (IC₅₀)

HDAC-10

21 μM (IC₅₀)

HDAC-9

50 μM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	7.8 nM Compound: 9; 4SC-202	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37487305]
D283 Med	IC₅₀	150 nM Compound: 18	Antiproliferative activity against human D283 Med cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human D283 Med cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay	[PMID: 37989059]

In Vitro

Domatinostat (4SC-202 free base) tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC₅₀ 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity^[1]. Domatinostat (4SC-202 free base) tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat (4SC-202 free base) tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat (4SC-202 free base) tosylate induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat tosylate. Domatinostat (4SC-202 free base) tosylate-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 tosylate in HT-29 cells. Notably, Domatinostat (4SC-202 free base) tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity^[2]. Domatinostat (4SC-202 free base) tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat (4SC-202 free base) tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral gavage of Domatinostat (4SC-202 free base) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 910462-43-0
Appearance Solid
Molecular Weight 447.51
Formel C₂₃H₂₁N₅O₃S
Color Off-white to yellow
SMILES

O=C(NC1=CC=CC=C1N)/C=C/C2=CN(S(=O)(C3=CC=C(C4=CN(C)N=C4)C=C3)=O)C=C2
Synonyms

4SC-202 free base
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.
Am J Transl Res

4SC-202 induces apoptosis in myelodysplastic syndromes and the underlying mechanism. [Abstract]

2020 Jun 15;12(6):2968-2983. PMID: 32655823

Domatinostat purchased from MedChemExpress. Usage Cited in: Am J Transl Res. 2020 Jun 15;12(6):2968-2983. [Abstract]

Western blot analyzes that the expression levels of LSD1, HDAC1/2/3, BCL-2 and CDK1 proteins are decreased and the expression levels of H3K4me2, AC-H3, cleavage caspase3/9, BAX, and p21 proteins are significantly increased by 4SC-202.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 58 mg/mL (129.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2346 mL

11.1729 mL

22.3459 mL

5 mM

0.4469 mL

2.2346 mL

4.4692 mL

10 mM

0.2235 mL

1.1173 mL

2.2346 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pinkerneil M, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines. Target Oncol. 2016 Dec;11(6):783-798. [Content Brief]

[2]. Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67. [Content Brief]

[3]. Fu M, et al. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73 [Content Brief]

[4]. S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2346 mL	11.1729 mL	22.3459 mL	55.8647 mL
	5 mM	0.4469 mL	2.2346 mL	4.4692 mL	11.1729 mL
	10 mM	0.2235 mL	1.1173 mL	2.2346 mL	5.5865 mL
	15 mM	0.1490 mL	0.7449 mL	1.4897 mL	3.7243 mL
	20 mM	0.1117 mL	0.5586 mL	1.1173 mL	2.7932 mL
	25 mM	0.0894 mL	0.4469 mL	0.8938 mL	2.2346 mL
	30 mM	0.0745 mL	0.3724 mL	0.7449 mL	1.8622 mL
	40 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	50 mM	0.0447 mL	0.2235 mL	0.4469 mL	1.1173 mL
	60 mM	0.0372 mL	0.1862 mL	0.3724 mL	0.9311 mL
	80 mM	0.0279 mL	0.1397 mL	0.2793 mL	0.6983 mL
	100 mM	0.0223 mL	0.1117 mL	0.2235 mL	0.5586 mL

Keywords

Domatinostat

4 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Domatinostat

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Domatinostat Related Classifications

HY-16012A Related Classifications