Domatinostat (4SC-202)

For research use only.

Catalog No.S7555

5 publications

Domatinostat (4SC-202) Chemical Structure

CAS No. 910462-43-0

Domatinostat (4SC-202) 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. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.

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Selleck's Domatinostat (4SC-202) has been cited by 5 publications

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Biological Activity

Description Domatinostat (4SC-202) 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. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
Targets
HDAC3 [1]
(Cell-free assay)		 HDAC2 [1]
(Cell-free assay)		 HDAC1 [1]
(Cell-free assay)		 HDAC11 [1]
(Cell-free assay)		 HDAC5 [1]
(Cell-free assay)
0.57 μM 1.12 μM 1.20 μM 9.7 μM 11.3 μM
In vitro

In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CRL-2105 NFnkS4ZE\WyuII\pZYJqdGm2eTDhd5NigQ>? MUG3NwKBkWh? M3nxeWlEPTB;MUewJI5O NYL3ZpozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>
MyLa M4jKVmNmdGxidnnhZoltcXS7IHHzd4F6 MmjYO|LjiImq M3ntc2lEPTB;MUmwJI5O NETyN5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEi4OVI2OCd-M{C4PFUzPTB:L3G+
CRL-8294 MVLD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NIizflU4OuLCiXi= MX7JR|UxRTJ4MDDuUS=> NYS4b|N{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>
HTB-176 MVPD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NI\SW5g4OuLCiXi= MVPJR|UxRTN5MDDuUS=> NWHUUmExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>
Se-Ax MnPJR4VtdCC4aXHibYxqfHliYYPzZZk> NUDGcVZnPzMkgJno M2rIdGlEPTB;MkWwJI5O M2XuU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOEi1NlUxLz5|MEi4OVI2ODxxYU6=
HuT 78 NHPuNYVE\WyuII\pZYJqdGm2eTDhd5NigQ>? M2\GRVcz6oDLaB?= NG\JfFNKSzVyPUOzNEBvVQ>? NGDJNWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEi4OVI2OCd-M{C4PFUzPTB:L3G+

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
Ac α-tubulin / Ac Histone H3 / Ac Histone H4 ; 

PubMed: 27250763     


Levels of acetylated α-tubulin and histone H3 and H4 were quantified in VM-CUB1 and UM-UC-3 cells after defined 4SC-202 treatment (0.5/2.5 μM, 24/48 h). Treatment with 3 nM romidepsin served as positive control for H3 and H4 acetylation; treatment with 2.5 μM SAHA served as a positive control for acetylated α-tubulin. DMSO was the solvent control.

Cyclin A / Cyclin B1 / Cyclin D1 / Cyclin E / p21 ; 

PubMed: 27250763     


Cyclins (A, B1, D1, E) and p21 protein expression levels following 4SC-202 (0.5/2.5 μM) or 2.5 μM SAHA treatment were quantified by western blot analysis in comparison to DMSO treatment in VM-CUB1 and UM-UC-3 cells (24/48 h)

Caspase-3 / Cleaved Caspase-3 / H3K4me2 / H3K9ac ; 

PubMed: 30885250     


Total cell lysates harvested after 48 h of drug treatment were subjected to immunoblot analysis using antibodies recognizing the indicated targets (H3K4me2: histone H3 dimethyl lysine 4; H3K9ac: histone H3 acetyl lysine 9)

27250763 30885250
Growth inhibition assay
Cell viability ; 

PubMed: 27250763     


UCCs and control cells were treated with increasing amounts of the class I HDAC specific inhibitor 4SC-202. The dose–response curves after 72 h 4SC-202 treatment are shown exemplarily for the UCCs VM-CUB1 and UM-UC-3 and the non-urothelial control cells HBLAK and HEK-293.

IC50; 

PubMed: 30885250     


IC50 doses for 4SC-202 and FK228-treated cells were calculated by nonlinear fitting of the MTS data

27250763 30885250
In vivo In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. [1]

Protocol

Cell Research:

[1]
- Collapse
  • Cell lines: CRC lines (HT-29, HCT-116, HT-15, and DLD-1)
  • Concentrations: 0.1, 1, 5, 10 μM
  • Incubation Time: 72 hours
  • Method:

    CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), the primary human colon cancer cells, or primary human colon epithelial cells were treated with applied concentrations of 4SC-202, cells were further cultured for indicated time, and cell survival was tested by MTT assay or trypan blue staining assay; cell proliferation was tested by clonogenicity assay. Expression of listed proteins was tested by Western blots.


    (Only for Reference)
Animal Research:

[1]
- Collapse
  • Animal Models: A549 NSCLC xenograft model and RKO27 colon carcinoma model
  • Dosages: 120 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (198.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 447.51
Formula

C23H21N5O3S
CAS No. 910462-43-0
Storage powder
in solvent
Synonyms
Smiles CN1C=C(C=N1)C2=CC=C(C=C2)S(=O)(=O)N3C=CC(=C3)C=CC(=O)NC4=CC=CC=C4N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01344707 Completed Drug: 4SC-202 Advanced Hematologic Malignancies 4SC AG March 2011 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Do you have suggestions about the in vivo formulation of the compound?

  • Answer:

    For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O with solubility up to 10mg/ml.

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID