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LKB1 (AAK1 dual inhibitor)

现货
Catalog No.
A3556
Pim-1激酶抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,240.00
现货
10mg
¥ 2,880.00
现货
50mg
¥ 7,040.00
现货
200mg
¥ 19,710.00
现货

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Background

LKB1 is a selective inhibitor of Pim-1 kinase with Kd value of 35 nM [1].
Pim-1 (proto-oncogene serine/threonine-protein kinase) is a proto-oncogene encodes by PIM1 gene and is reported to play an important role in multiple human cancers. Initially, pim-1 is reported to be expressed in spleen, thymus, bone marrow, prostate, oral epithelial cells, etc. Recently, the high expression of pim-1 has been identified in several isolated human cancer cells and been shown to involve in the cell cycle progression, apoptosis, transcriptional activation and many general signal transduction pathways. Therefore, investigation of the inhibition of pim-1 by low molecular weight compounds as a part of anticancer therapeutic strategies needs more attention and progress [2, 3].
References:
1.    Bamborough, P., et al., Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem, 2008. 51(24): p. 7898-914.
2.    Natarajan, K., et al., The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms. Biochem Pharmacol, 2013. 85(4): p. 514-24.
3.    Tsuganezawa, K., et al., A novel Pim-1 kinase inhibitor targeting residues that bind the substrate peptide. J Mol Biol, 2012. 417(3): p. 240-52.

Chemical Properties

StorageStore at -20°C
M.Wt339.36
Cas No.1093222-27-5
FormulaC20H13N5O
SynonymsLKB1/AAK1 dual inhibitor
Solubility≥34.8 mg/mL in DMSO, <1.76 mg/mL in H2O, <1.7 mg/mL in EtOH
Chemical NameN-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide
SDFDownload SDF
Canonical SMILESC1=CC(=CN=C1)C(=O)NC2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)C#N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

结合实验

将激酶作为融合蛋白表达在T7噬菌体中,通常情况下,全长构建体用于小激酶和大激酶的催化结构域。将T7-激酶标记的噬菌体菌株与固定在链霉素包被的磁珠上的已知激酶抑制剂以及单一浓度10 μM的LKB1 (AAK1 dual inhibitor)混合。定量PCR检测结果表明,LKB1 (AAK1 dual inhibitor)与激酶ATP位点结合,取代激酶/噬菌体的固定配体,结果表示为相对于对照组DMSO的激酶/噬菌体结合至配体/磁珠的百分比。高亲和力化合物具有对照比为0,而较弱的结合剂具有较高的对照百分比。这些是针对203种人激酶筛选的结果。

References:

[1]. Bamborough P, Drewry D, Harper G, et al. Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem, 2008, 51(24): 7898-7914.

质量控制

化学结构

LKB1 (AAK1 dual inhibitor)