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IRAK-1-4 Inhibitor I

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Chemical Structure| 509093-47-4 同义名 : IRAK-1/4 Inhibitor I;IRAK-1/4 Inhibitor
CAS号 : 509093-47-4
货号 : A496272
分子式 : C20H21N5O4
纯度 : 99%+
分子量 : 395.412
MDL号 : MFCD09752602
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(10.12 mM)，配合低频超声，并调节pH至3，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 25 mg/mL(63.23 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 IRAK-1-4 Inhibitor I has IC50 greater than the highest concentration tested (10 μM) against a panel of 27 other kinases, including the most closely homologous (outside of the IRAK family) Lck and pp60SRC. Additionally, IRAK-1-4 Inhibitor I does not show any signs of cytotoxicity in a 72 h proliferation assay in HeLa cells (ED50>30 μM). Significant inhibition of IRAK-1 is observed with IRAK-1-4 Inhibitor I (IRAK-1 IC50=0.3 μM)[1]. The IRAK-1/4 inhibitor suppresses LPS-induced elevations in Bcl10, NF-κB, and IL-8. It mediates the LPS-induced activation of IL-8 and operates upstream of Bcl10. Following treatment, Bcl10 levels decrease by 73% (from 5.18±0.22 to 2.36±0.08 ng/mL), and IL-8 levels drop by 60% (from 2.64±0.31 to 1.14±0.08 ng/mL)[2].
作用机制 IRAK-1-4 Inhibitor I plays the role of IRAK-4 inhibitor by binding with acyl-2-aminobenzimidazole scaffold that represents a unique kinase binding motif.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.65mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL
参考文献

[1]Powers JP, et al. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2842-2845.

[2]Bhattacharyya S, et al. Bcl10 mediates LPS-induced activation of NF-kappaB and IL-8 in human intestinal epithelial cells. Am J Physiol Gastrointest Liver Physiol. 2007 Aug;293(2):G429-37.