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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) | $109 | In Stock |
Description | Domatinostat tosylate (4SC-202) is a selective inhibitor of class I HDAC for HDAC1/2/3 (IC50: 1.20/1.12/0.57 μM). It also displays inhibitory activity against 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]. |
Alias | 4SC-202 tosylate, 4SC-202 |
Molecular Weight | 619.71 |
Formula | C30H29N5O6S2 |
Cas No. | 1186222-89-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||
Solubility Information | DMSO: 50 mg/mL (80.68 mM) ![]() H2O: Insoluble | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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