Acalisib (GS-9820)
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.
Acalisib(GS-9820)是PI3Kδ的强效选择性抑制剂,IC50值为12.7 nM[1].
磷酸肌醇3-激酶(PI3Ks)属于脂激酶家族,磷酸化磷脂酰肌醇-4,5-二磷酸(PIP2)的3'-羟基基团以生成磷脂酰肌醇-3,4,5-三磷酸酯(PIP3).PI3Ks在细胞增殖\存活\分化和代谢中发挥重要作用.PI3Kδ在炎症\免疫功能\细胞迁移和囊泡运输中起重要作用,并且在造血起源的细胞中高表达[1].
Acalisib (GS-9820)是PI3Kδ的强效选择性抑制剂.GS-9820抑制PI3Kα\β\γ和δ的IC50值分别为5441\3377\1389和12.7 nM.在成纤维细胞中,GS-9820可抑制PDGF和LPA诱导的pAkt,IC50值分别为11,585和2069 nM,这是通过PI3Kα和PI3Kβ起作用的.在嗜碱性粒细胞中,GS-9820抑制FcεRI PI3Kδ-和fMLP PI3Kγ介导的CD63表达,EC50值分别为14 nM和2,065 nM.在离体大鼠破骨细胞中,GS-9820处理1015分钟诱导65-75％板状伪足及时回缩.GS-9820也显著减少F-肌动蛋白带的发生率,并抑制RANKL刺激的破骨细胞存活[1].
参考文献：
[1]. Shugg RP, Thomson A, Tanabe N, et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption. J Biol Chem, 2013, 288(49): 35346-35357.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 401.4 |
| Cas No. | 870281-34-8 |
| Formula | C21H16FN7O |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL in DMSO |
| Chemical Name | (S)-2-(1-((9H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one |
| SDF | Download SDF |
| Canonical SMILES | C[C@@](NC1=NC=NC2=C1N=CN2)([H])C(N3C4=CC=CC=C4)=NC5=C(C3=O)C=C(F)C=C5 |
| 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
- 批次:
化学结构
