Domatinostat (4SC-202)
For research use only. Not for use in humans.
Catalog No.S7555 Synonyms: Domatinostat
1 publication
Molecular Weight(MW): 447.51
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.
Selleck's Domatinostat (4SC-202) has been cited by 1 publication
Purity & Quality Control
Choose Selective HDAC Inhibitors
Biological Activity
| Description | 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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| 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] |
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| Cell Data |
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| Assay |
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| 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: |
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Solubility (25°C)
| In vitro | DMSO | 89 mg/mL (198.87 mM) |
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| 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 |
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| Formula | C23H21N5O3S |
| CAS No. | 910462-43-0 |
| Storage | powder |
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| Synonyms | Domatinostat |
| Smiles | C[N]1C=C(C=N1)C2=CC=C(C=C2)[S](=O)(=O)[N]3C=CC(=C3)\C=C\C(=O)NC4=CC=CC=C4N |
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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.
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Frequently Asked Questions
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Question 1:
Do you have suggestions about the in vivo formulation of the compound?
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Answer:
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O with solubility up to 10mg/ml.
