GSK1070916
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.
GSK1070916是一种有效的Aurora B/C激酶选择性抑制剂,Ki值分别为0.38 nM和1.5 nM[1]。
GSK1070916是一种可逆的ATP竞争性Aurora B和Aurora C抑制剂,Ki值分别为0.38 nM和1.5 nM。SPA试验表明,与Aurora A相比,GSK1070916对Aurora B/C具有良好的选择性。该物质可抑制Aurora B,IC50值为5 nM,但是对于Aurora A为1259 nM。也有报道显示,使用GSK1070916可在A549人类肺癌细胞中抑制细胞增殖,EC50值为7 nM。此外,体外和体内试验均证明GSK1070916可抑制Aurora B的底物组蛋白H3的磷酸化。GSK1070916也可在HL-60肿瘤异种移植物小鼠中抑制肿瘤生长[1]。
参考文献:
[1] Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 507.63 |
Cas No. | 942918-07-2 |
Formula | C30H33N7O |
Solubility | ≥25.4 mg/mL in DMSO |
Chemical Name | 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea |
SDF | Download SDF |
Canonical SMILES | CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC(=CC=C5)CN(C)C |
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。 |
Description | GSK1070916是一种可逆的ATP竞争性Aurora B和C的抑制剂,IC50值分别为3.5 nM和6.5 nM。 | |||||
靶点 | Aurora B | Aurora C | ||||
IC50 | 3.5 nM | 6.5 nM |