BX517(PDK1 inhibitor2)
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.
BX-517是PDK1的强效选择性抑制剂,与蛋白质的ATP结合口袋结合,IC50为6 nM.BX-517也阻断肿瘤细胞中Akt的活化,比其类似物在最高剂量(10 μM)下的效能强10倍,IC50为0.1–1.0 μM[1].磷酸肌醇依赖性激酶-1 (PDK1)是一种丝氨酸/苏氨酸激酶,是AGC激酶超家族一系列蛋白激酶的关键激活剂,在癌症发生和Akt\S6激酶以及蛋白激酶C的活化中发挥关键作用[2].
参考文献：
1. Islam I, Brown G, Bryant J et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25.
2. Islam I, Bryant J, Chou YL etc. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 282.3 |
| Cas No. | 850717-64-5 |
| Formula | C15H14N4O2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥8.55 mg/mL in DMSO |
| Chemical Name | (Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid |
| SDF | Download SDF |
| Canonical SMILES | C/C(C1=CC=CN1)=C(C(O)=N2)\C3=C2C=CC(NC(O)=N)=C3 |
| 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。 |
质量控制和MSDS
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化学结构
