LKB1 (AAK1 dual inhibitor)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LKB1是一种选择性的 Pim-1激酶抑制剂,Kd值为35 nM[1]。
PIM-1(原癌基因丝氨酸/苏氨酸-蛋白激酶)是由PIM1基因编码的酶,在多种人类癌症中具有重要作用。据报道,pim-1在脾脏、胸腺、骨髓、前列腺和口腔上皮细胞等部位表达。Pim-1在多个分离的人类肿瘤细胞中高表达,并参与细胞周期进程、细胞凋亡、转录激活和许多基本的信号转导途径。因此,抑制pim-1的低分子量化合物可用于抗癌治疗,需要得到更多的关注和发展[2,3]。
参考文献:
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.
Storage | Store at -20°C |
M.Wt | 339.36 |
Cas No. | 1093222-27-5 |
Formula | C20H13N5O |
Synonyms | LKB1/AAK1 dual inhibitor |
Solubility | insoluble in EtOH; insoluble in H2O; ≥34.8 mg/mL in DMSO |
Chemical Name | N-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1=CC(=CN=C1)C(=O)NC2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)C#N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
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