Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。它也抑制组蛋白赖氨酸特异性脱甲基酶1 的活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 322 | 现货 | ||
2 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 689 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,380 | 现货 | ||
100 mg | ¥ 5,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 958 | 现货 |
产品描述 | 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). |
靶点活性 | HDAC1:1.2 μM, HDAC10:21 μM, HDAC11:9.7 μM, HDAC3:0.57 μM, HDAC5:11.3 μM, HDAC2:1.12 μM |
体外活性 | 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]. |
体内活性 | 4SC-202 (i.g.) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2]. |
别名 | 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
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6137 mL | 8.0683 mL | 16.1366 mL | 40.3415 mL |
5 mM | 0.3227 mL | 1.6137 mL | 3.2273 mL | 8.0683 mL | |
10 mM | 0.1614 mL | 0.8068 mL | 1.6137 mL | 4.0341 mL | |
20 mM | 0.0807 mL | 0.4034 mL | 0.8068 mL | 2.0171 mL | |
50 mM | 0.0323 mL | 0.1614 mL | 0.3227 mL | 0.8068 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Domatinostat tosylate 1186222-89-8 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Domatinostat 4SC202 4SC-202 Tosylate 4SC-202 tosylate inhibit Histone deacetylases Inhibitor 4SC202 Tosylate Domatinostat Tosylate 4SC 202 Tosylate 4SC-202 4SC 202 inhibitor