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Domatinostat (4SC202) 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.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $35 | In Stock | |
| 5 mg | $81 | In Stock | |
| 10 mg | $123 | In Stock | |
| 25 mg | $228 | In Stock | |
| 50 mg | $372 | In Stock | |
| 100 mg | $558 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $89 | In Stock |
| Description | Domatinostat (4SC202) 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&IC50 | HDAC1:1.20 μM, HDAC3:0.57 μM, HDAC10:21 μM, HDAC5:11.3 μM, HDAC11:9.7 μM, HDAC2:1.12 μM, HDAC9:50 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] |
| 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] |
| Synonyms | 4SC-202 (free base), 4SC-202, 4SC202, 4SC 202 |
| Molecular Weight | 447.51 |
| Formula | C23H21N5O3S |
| Cas No. | 910462-43-0 |
| Smiles | Cn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1 |
| Relative Density. | 1.34 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 82 mg/mL (183.24 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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