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Domatinostat (4SC202) 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 的活性。
Domatinostat (4SC202) 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 的活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 188 | 现货 | |
5 mg | ¥ 568 | 现货 | |
10 mg | ¥ 928 | 现货 | |
25 mg | ¥ 1,730 | 现货 | |
50 mg | ¥ 2,780 | 现货 | |
100 mg | ¥ 3,990 | 现货 | |
200 mg | ¥ 5,680 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 627 | 现货 |
产品描述 | Domatinostat (4SC202) 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. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. |
靶点活性 | HDAC2:1.12 μM, HDAC3:0.57 μM, HDAC1:1.20 μM |
体外活性 | In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. [1] |
体内活性 | In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. [1] |
别名 | 4SC-202 (free base), 4SC-202, 4SC202, 4SC 202 |
分子量 | 447.51 |
分子式 | C23H21N5O3S |
CAS No. | 910462-43-0 |
Smiles | Cn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1 |
密度 | 1.34 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 82 mg/mL (183.24 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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