for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at 2-8°C,Desiccated Ships Wet ice 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.
Form:Solid
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Classe | Azoles |
| Subclass | Pyrazoles |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenylpyrazoles |
| Alternative Parents | p-Methylbenzenesulfonates Tosyl compounds 2'-Aminoanilides Benzenesulfonamides 1-sulfo,2-unsubstituted aromatic compounds Benzenesulfonyl compounds N-arylamides Aniline and substituted anilines Substituted pyrroles Sulfonyls Organosulfonic acids Heteroaromatic compounds Secondary carboxylic acid amides Amino acids and derivatives Azacyclic compounds Carbonyl compounds Hydrocarbon derivatives Organic oxides Primary amines |
| Molecular Framework | Not available |
| Substituents | Phenylpyrazole - P-methylbenzenesulfonate - 2'-aminoanilide - Benzenesulfonamide - Tosyl compound - Benzenesulfonate - Arylsulfonic acid or derivatives - Benzenesulfonyl group - Anilide - 1-sulfo,2-unsubstituted aromatic compound - Aniline or substituted anilines - N-arylamide - Toluene - Monocyclic benzene moiety - Substituted pyrrole - Benzenoid - Pyrrole - Heteroaromatic compound - Organic sulfonic acid or derivatives - Organosulfonic acid or derivatives - Organosulfonic acid - Sulfonyl - Secondary carboxylic acid amide - Carboxamide group - Amino acid or derivatives - Carboxylic acid derivative - Azacycle - Amine - Primary amine - Hydrocarbon derivative - Organosulfur compound - Organooxygen compound - Organonitrogen compound - Carbonyl group - Organic nitrogen compound - Organic oxygen compound - Organic oxide - Aromatic heteromonocyclic compound |
| Descrizione | This compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group. |
| External Descriptors | Not available |
| Solubilità | DMSO : ≥ 51 mg/mL (82.30 mM) |
|---|---|
| Peso molecolare | 619.700 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 7 |
| Exact Mass | 619.156 Da |
| Monoisotopic Mass | 619.156 Da |
| Topological Polar Surface Area | 183.000 Ų |
| Heavy Atom Count | 43 |
| Formal Charge | 0 |
| Complexity | 981.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 1 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 1 |
| Covalently-Bonded Unit Count | 2 |
