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IRAK-1-4 Inhibitor I 是一种IRAK1/4双重抑制剂,其IC50分别为 0.2 μM 和 0.3 μM。
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IRAK-1-4 Inhibitor I 是一种IRAK1/4双重抑制剂,其IC50分别为 0.2 μM 和 0.3 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 297 | 现货 | |
2 mg | ¥ 433 | 现货 | |
5 mg | ¥ 685 | 现货 | |
10 mg | ¥ 938 | 现货 | |
25 mg | ¥ 1,860 | 现货 | |
50 mg | ¥ 3,150 | 现货 | |
100 mg | ¥ 4,480 | 现货 | |
500 mg | ¥ 9,330 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 693 | 现货 |
产品描述 | IRAK-1-4 Inhibitor I is a dual inhibitor of IRAK4 and IRAK1. |
靶点活性 | IRAK4:0.3 μM, IRAK1:0.2 μM |
体外活性 | IRAK-1-4抑制剂I对27种其他激酶的IC50值均大于最高测量浓度(10 μM),包括最接近的同源激酶(非IRAK家族) Lck和pp60SRC。此外,在72小时HeLa细胞增殖实验中,IRAK-1-4抑制剂I未展现出任何细胞毒性迹象(ED50>30 μM)。显著地,IRAK-1的抑制在IRAK-1-4抑制剂I作用下观察到(IRAK-1 IC50=0.3 μM)[1]。IRAK-1/4抑制剂能够消除LPS诱导的Bcl10、NF-κB和IL-8的增加。IRAK-1/4介导LPS诱导的IL-8激活并位于Bcl10上游。LPS诱导的Bcl10增加量下降了73%(从5.18±0.22下降至2.36±0.08 ng/mL),IL-8反应下降了60%(从2.64±0.31下降至1.14±0.08 ng/mL)[2]。 |
激酶实验 | Kinase Assays: Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1. |
细胞实验 | IRAK-1-4 Inhibitor I is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. NCM460 cells, grown in 24-well plates, are incubated with 50 μM IRAK-1/4 inhibitor for 2 h. After 2 h, the media are changed, and new media with or without LPS (10 ng/mL) added. Treatment is terminated at 6 h, and spent media and cells are collected for IL-8 and other assays[2]. |
别名 | IRAK-1/4 Inhibitor I, IRAK-1/4 Inhibitor |
分子量 | 395.41 |
分子式 | C20H21N5O4 |
CAS No. | 509093-47-4 |
Smiles | [O-][N+](=O)c1cccc(c1)C(=O)Nc1nc2ccccc2n1CCN1CCOCC1 |
密度 | 1.40 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: 8.13 mg/mL (20.55 mM), Sonication is recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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