CCG-63802
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.
CCG-63802是一种选择性的RGS4抑制剂,IC50值为1.9 μM [1]。
RGS(G蛋白信号传导的调节因子)是多功能的GTP酶加速蛋白,并在通过异源G蛋白α亚基促进GTP水解中起着重要的作用。RGS4也被称为RGP4,并对信号传导上游负调节或异源G蛋白的水平起关键作用[1,2]。
CCG-63802是一种强效的RGS抑制剂,不同于已报道的RGS4不可逆抑制剂CCG-4986。使用[32P]GTP单转换GAP试验表明,CCG-63802治疗抑制RGS4的GAP活性[1]。用HEK-293细胞测试时,CCG-63802给药通过抑制RGS4,成功逆转8-Br-cGMP对BK的抑制作用[2]。
参考文献:
[1]. Blazer, L.L., et al., Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol, 2010. 78(3): p. 524-33.
[2]. Dobrivojevic, M., et al., Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol, 2012. 303(12): p. C1260-8.
Physical Appearance | Yellow solid |
Storage | Store at -20°C |
M.Wt | 450.52 |
Cas No. | 620112-78-9 |
Formula | C26H18N4O2S |
Synonyms | CCG 63802;CCG63802 |
Solubility | Limited solubility, soluble in DMSO |
Chemical Name | (E)-2-(1,3-benzothiazol-2-yl)-3-[9-methyl-2-(3-methylphenoxy)-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile |
SDF | Download SDF |
Canonical SMILES | CC1=CC(=CC=C1)OC2=C(C(=O)N3C=CC=C(C3=N2)C)C=C(C#N)C4=NC5=CC=CC=C5S4 |
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。 |