| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S82234-1mg |
≥98% | ￥320.00 |
货期：3-5天 | - | - | - | - |
|
S82234-2mg |
≥98% | ￥460.00 |
货期：3-5天 | - | - | - | - |
|
S82234-5mg |
≥98% | ￥680.00 |
货期：3-5天 | - | - | - | - |
|
S82234-10mg |
≥98% | ￥1120.00 |
货期：3-5天 | - | - | - | - |
|
S82234-25mg |
≥98% | ￥2050.00 |
货期：3-5天 | - | - | - | - |
|
S82234-50mg |
≥98% | ￥3300.00 |
货期：3-5天 | - | - | - | - |
|
S82234-100mg |
≥98% | ￥5300.00 |
货期：3-5天 | - | - | - | - |
|
| 产品描述： | Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 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). | ||||||||||||||||||||
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| 靶点： | HDAC-3:0.57 μM (IC50);HDAC-2:1.12 μM (IC50);HDAC-1:1.2 μM (IC50);HDAC-11:9.7 μM (IC50);HDAC-5:11.3 μM (IC50);HDAC-10:21 μM (IC50);HDAC-9:50 μM (IC50);Apoptosis; HDAC | ||||||||||||||||||||
| 体外研究： | 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 | ||||||||||||||||||||
| 体内研究： | Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened | ||||||||||||||||||||
| 参考文献： | 1. Pinkerneil M, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines. Target Oncol. 2016 Dec;11(6):783-798. 2. S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor. 3. Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67. 4. Fu M, et al. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73 | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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北京