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Pyroxamide 是一种组蛋白脱乙酰基酶 1 抑制剂,IC50为 100 nM。 它可以诱导白血病细胞凋亡和细胞周期停滞。
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Pyroxamide 是一种组蛋白脱乙酰基酶 1 抑制剂,IC50为 100 nM。 它可以诱导白血病细胞凋亡和细胞周期停滞。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 185 | 现货 | |
5 mg | ¥ 413 | 现货 | |
10 mg | ¥ 690 | 现货 | |
25 mg | ¥ 1,490 | 现货 | |
50 mg | ¥ 2,220 | 现货 | |
100 mg | ¥ 3,280 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Pyroxamide is an histone deacetylases (HDACs) inhibitor with antineoplastic properties ( HDAC1;IC50: 0.1-0.2 μM). |
靶点活性 | HDAC1:0.1-0.2 μM |
体外活性 | Pyroxamide作为HDACs抑制剂的活性。Pyroxamide在亚微摩尔浓度下抑制了经亲和纯化的HDAC1的酶活性。Pyroxamide抑制HDAC1活性的ID50值约为100 nm。与Pyroxamide (4 μm) 共培养4、24或48小时的MEL细胞显示出H2A、H2B、H3和H4乙酰化组蛋白的积累。而未与该试剂共培养的细胞在相同时间点上乙酰化组蛋白的基础水平较低[1]。 |
体内活性 | Pyroxamide可能是治疗恶性肿瘤的有效药物,其通过在转化细胞中诱导p21/WAF1表达,从而可能对该药物的抗肿瘤效应做出贡献[1]。 |
细胞实验 | HDAC1 enzyme assay, ?A MEL cell line expressing the epitope Flag-tagged HDAC1 was generated.?HDAC1-Flag was affinity purified by immunoprecipitation using M2 anti-Flag antibody-coated agarose, followed by elution from the agarose using the Flag peptide.?[3H]acetate-labeled cellular histones were prepared from MEL cells and were used as a substrate for the HDAC activity assay.?Released [3H]acetic acid was quantified by scintillation counting.?For inhibition studies, the enzyme preparations were preincubated with pyroxamide (10 to 100,000 nm) for 30 min at 4°C.[1] |
分子量 | 265.31 |
分子式 | C13H19N3O3 |
CAS No. | 382180-17-8 |
Smiles | ONC(=O)CCCCCCC(=O)Nc1cccnc1 |
密度 | 1.215 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 125 mg/mL (471.15 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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