GSK481
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.
作用于RIP1,IC50为1.3 nM。
GSK481是一种受体相互作用蛋白激酶1(RIP1)抑制剂。
RIP1激酶在肿瘤坏死因子介导的炎症中的作用使其成为治疗多种炎性疾病的有希望的靶点。
体外:先前的研究表明,在U937细胞测定中,GSK481不仅可以引发生化活性的增加,而且表现出极大的翻译,IC50为10 nM。此外,用P33放射性标记筛选测定分析时,针对其他所有测试激酶,GSK481还显示对RIP1激酶的完全特异性。在ATP浓度增加的紧密结合ADP-Glo IC50测定中,GSK481效力转低,对应于竞争性模型。此外,GSK481是野生型人RIP1中S166磷酸化的强效抑制剂,但对于降低野生型小鼠RIP1的S166磷酸化无效。 GSK481还能够在所有三种测试的小鼠RIP1突变体中比在野生型小鼠中更强效地抑制Ser166磷酸化[1]。
体内:迄今为止,尚无GSK481动物体内报告数据。
临床试验:到目前为止,GSK481仍处于临床前研究阶段。
参考文献:
[1] Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 377.39 |
Cas No. | 1622849-58-4 |
Formula | C21H19N3O4 |
Solubility | Soluble in DMSO |
Chemical Name | (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O |
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。 |