Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
説明 | 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). |
ターゲット&IC50 | HDAC1:1.2 μM, HDAC10:21 μM, HDAC11:9.7 μM, HDAC3:0.57 μM, HDAC5:11.3 μM, HDAC2:1.12 μM |
In vitro | 4SC-202 provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate 4SC-202-exerted cytotoxicity in CRC cells. Meanwhile, 4SC-202 induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of 4SC-202. 4SC-202-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 4SC-202 in HT-29 cells. Notably, 4SC-202, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. 4SC-202 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]. 4SC-202 treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. 4SC-202 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]. |
別名 | 4SC-202 tosylate, 4SC-202 |
分子量 | 619.71 |
分子式 | C30H29N5O6S2 |
CAS No. | 1186222-89-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (80.68 mM)
H2O: Insoluble
You can also refer to dose conversion for different animals. 詳細
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