10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Desiccated,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC 50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1 , HDAC2 , and HDAC3 , respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1) .
In Vitro
Domatinostat tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC 50 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity. Domatinostat tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat tosylate induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat tosylate. Domatinostat tosylate-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat tosylate in HT-29 cells. Notably, Domatinostat tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity. Domatinostat tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Isomeric SMILES | CC1=CC=C(C=C1)S(=O)(=O)O.CN1C=C(C=N1)C2=CC=C(C=C2)S(=O)(=O)N3C=CC(=C3)/C=C/C(=O)NC4=CC=CC=C4N |
|---|---|
| Alternate CAS | 1186222-89-8 |
| PubChem CID | 44217246 |
| MeSH Entry Terms | 4SC-202;domatinostat |
| Molecular Weight | 619.71 |
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