| Name | Domatinostat tosylate |
| Description | Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor targeting HDAC1/2/3 with IC50 values of 1.20/1.12/0.57 μM, respectively, and also inhibits Lysine-specific demethylase 1 (LSD1). |
| In vitro | Domatinostat provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat. Domatinostat-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 in HT-29 cells. Notably, Domatinostat, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. Domatinostat obviously reduces the proliferation of all epithelial and mesenchymal UC cell lines (IC50: 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity[1]. Domatinostat treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D[3]. |
| In vivo | 4SC-202 (i.g.) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (80.68 mM), Sonication is recommended.
H2O : Insoluble
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| Keywords | HDAC9 | HDAC5 | HDAC3 | HDAC2 | HDAC11 | HDAC10 | HDAC1 | HDAC | Domatinostat | Apoptosis | 4SC202 Tosylate | 4SC202 | 4SC 202 Tosylate | 4SC 202 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | L-Ascorbic acid | L-Glutamic acid | Tributyrin | Valproic Acid | Curcumin | L-Ascorbic acid sodium salt | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Reprogramming Compound Library | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
