Home Epigenetics HDAC inhibitor Domatinostat (4SC-202) For research use only.

Domatinostat (4SC-202)

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

Domatinostat (4SC-202) Chemical Structure

CAS: 910462-43-0

Selleck's Domatinostat (4SC-202) has been cited by 12 publications

Purity & Quality Control

Batch: Purity: 99.9%
99.9

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CRL-2105 Cell viability assay 72 h IC50=170 nM 30885250
MyLa Cell viability assay 72 h IC50=190 nM 30885250
CRL-8294 Cell viability assay 72 h IC50=260 nM 30885250
HTB-176 Cell viability assay 72 h IC50=370 nM 30885250
Se-Ax Cell viability assay 72 h IC50=250 nM 30885250
HuT 78 Cell viability assay 72 h IC50=330 nM 30885250
Click to View More Cell Line Experimental Data

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 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 Research 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.
Experimental Result Images Methods Biomarkers Images 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
Growth inhibition assay Cell viability IC50 27250763
In Vivo
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]
Animal Research Animal Models A549 NSCLC xenograft model and RKO27 colon carcinoma model
Dosages 120 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01344707 Completed Advanced Hematologic Malignancies 4SC AG March 2011 Phase 1

Chemical lnformation & Solubility

Molecular Weight 447.51 Formula

C23H21N5O3S
CAS No. 910462-43-0 SDF Download Domatinostat (4SC-202) SDF
Smiles CN1C=C(C=N1)C2=CC=C(C=C2)S(=O)(=O)N3C=CC(=C3)C=CC(=O)NC4=CC=CC=C4N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (198.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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
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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.

HDAC Signaling Pathway Map

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