Home Epigenetics HDAC inhibitor Domatinostat (4SC-202)

Domatinostat (4SC-202)

Catalog No.S7555

For research use only.

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.

Domatinostat (4SC-202) Chemical Structure

CAS No. 910462-43-0

Selleck's Domatinostat (4SC-202) has been cited by 6 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)		 Click to View More Targets
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 MW\D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MorZO|LjiImq M4nQbGlEPTB;MUewJI5O MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODh6NUK1NEc,OzB6OEWyOVA9N2F-
MyLa NHXWSXpE\WyuII\pZYJqdGm2eTDhd5NigQ>? MX:3NwKBkWh? M4rGSmlEPTB;MUmwJI5O MmjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6OEWyOVAoRjNyOEi1NlUxRC:jPh?=
CRL-8294 M3H5R2NmdGxidnnhZoltcXS7IHHzd4F6 Mn;MO|LjiImq M4Wy[2lEPTB;Mk[wJI5O MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODh6NUK1NEc,OzB6OEWyOVA9N2F-
HTB-176 NVnIVVhOS2WubDD2bYFjcWyrdImgZZN{[Xl? MYe3NwKBkWh? MnzDTWM2OD1|N{Cgcm0> NUTzPZd3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>
Se-Ax NWXVdGVuS2WubDD2bYFjcWyrdImgZZN{[Xl? Mn2xO|LjiImq M4DoWmlEPTB;MkWwJI5O MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODh6NUK1NEc,OzB6OEWyOVA9N2F-
HuT 78 MmPlR4VtdCC4aXHibYxqfHliYYPzZZk> NFnTeY04OuLCiXi= M2HnUmlEPTB;M{OwJI5O Mn;TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6OEWyOVAoRjNyOEi1NlUxRC:jPh?=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot Ac α-tubulin / Ac Histone H3 / Ac Histone H4 ; Cyclin A / Cyclin B1 / Cyclin D1 / Cyclin E / p21 ; Caspase-3 / Cleaved Caspase-3 / H3K4me2 / H3K9ac 27250763 30885250
Growth inhibition assay Cell viability ; IC50 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 (from reference)

Cell Research:

[1]
  • 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.
Animal Research:

[1]
  • Animal Models: A549 NSCLC xenograft model and RKO27 colon carcinoma model
  • Dosages: 120 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 447.51
Formula

C23H21N5O3S
CAS No. 910462-43-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C=N1)C2=CC=C(C=C2)S(=O)(=O)N3C=CC(=C3)C=CC(=O)NC4=CC=CC=C4N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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