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Domatinostat tosylate

CAS No. : 1186222-89-8

MCE 站：Domatinostat tosylate

产品活性：Domatinostat tosylate (4SC-202) 是一种 I 型 HDAC 抑制剂，能够抑制 HDAC1，HDAC2，和 HDAC3 的活性，IC₅₀ 值分别为 1.20 μM，1.12 μM 和 0.57 μM；同时能够抑制组蛋白赖氨酸特异性脱甲基酶1 (Lysine specific demethylase 1) 的活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：HDAC  |  Apoptosis

In Vitro: Domatinostat tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC₅₀ 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.

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.

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