购物车
- 全部删除
- 您的购物车当前为空
ACHP Hydrochloride (IKK-2 Inhibitor VIII) 是选择性的IKK-β抑制剂 (IC50=5.8 nM)。
ACHP Hydrochloride (IKK-2 Inhibitor VIII) 是选择性的IKK-β抑制剂 (IC50=5.8 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 596 | 现货 | |
2 mg | ¥ 783 | 现货 | |
5 mg | ¥ 1,130 | 现货 | |
10 mg | ¥ 1,820 | 现货 | |
25 mg | ¥ 3,480 | 现货 | |
50 mg | ¥ 4,350 | 现货 | |
100 mg | ¥ 6,230 | 现货 | |
500 mg | ¥ 12,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,230 | 现货 |
产品描述 | ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM. |
靶点活性 | IKKα:250 nM, IKKβ:8.5 nM |
体外活性 | ACHP Hydrochloride展现出强效的IKK-β抑制作用(IC50:8.5 nM),以及显著的细胞内活性(IC50:40 nM,在A549细胞中)。ACHP对IKK-α具有适度抑制效果(IC50为250 nM),但对其他激酶如IKK3、Syk和MKK4则表现出良好的选择性(IC50>20,000 nM)。此化合物能抑制TNFα激活的HEK293细胞和PMA/钙离子载体激活的Jurkat T细胞中NF-κB依赖性报告基因的激活。然而在超过10μM的浓度下,ACHP未能抑制MRC-5细胞中PMA诱导的AP-1激活,也未能抑制Jurkat细胞中PMA/钙离子载体诱导的NF-κB依赖性报告基因转录。ACHP通过抑制活细胞中的IKK-β选择性干预NF-κB信号通路[1]。此化合物以剂量依赖方式抑制这些细胞的生长。Tax活跃细胞系对ACHP的敏感度高于Tax非活跃细胞系及Jurkat细胞(Tax活跃、非活跃细胞系或Jurkat细胞的IC50值分别为3.1±1.3μM、10.7±1.7μM和23.6μM),这表明Tax活跃细胞的生长更依赖NF-κB[2]。 |
体内活性 | ACHP在小鼠和大鼠体内具有可口服和生物利用度,并在抗炎模型中显示出显著的体内活性(花生四烯酸引起的小鼠耳肿炎模型)。ACHP在水中具有合理的溶解度(在pH 7.4的等渗缓冲液中为0.12 mg/mL)和优秀的Caco-2透过性(Papp 62.3×10^-7 cm/s)。ACHP在大鼠中的良好生物利用度可能归因于其低清除率(0.33 L/h/kg)。在急性炎症模型中,ACHP以1 mg/kg的剂量依赖性方式表现出口服有效性[1]。 |
细胞实验 | HTLV-1-infected T-cell lines, ATL-35T, 81-66/45, MJ, and MT-2 cells, human ATL cell lines established from ATL patients, ATL-102, ED-40515(?) and TL-Om1 cells, and an HTLV-1-negative T-cell leukemia cell line Jurkat are used in this study. Approximately 1.5×10^4 cells are cultured in 96-well plates in triplicates at 37°C. Growth inhibitory effect of ACHP (0.01, 0.1, 1, 5, 10, 50 and 100 μM) is determined using MTT assay. Optical densities (OD) at 570 and 630?nm are measured with a multi-plate reader. Cell viability (%) is calculated [2]. |
动物实验 | In vivo arachidonic acid-induced ear edema in mice: ear edema is induced by topical application of arachidonic acid (500 μg/ear). ACHP (0.3, 1 and 3 mg/kg, p.o.), Dexamethasone, and vehicle (10% cremophor in saline) are given po 60 min before the arachidonic acid application. Ear thickness is measured at 0, 1, 3, and 6 h after the arachidonic acid application [1]. |
别名 | IKK-2 Inhibitor VIII |
分子量 | 400.9 |
分子式 | C21H25ClN4O2 |
CAS No. | 406209-26-5 |
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: 45 mg/mL (112.25 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.