推荐产品
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(NC1=CC=C(NN=C2)C2=C1)C3=C(C)NC(NC3C4=CC=C(F)C=C4)=O
InChI
1S/C19H16FN5O2/c1-10-16(17(24-19(27)22-10)11-2-4-13(20)5-3-11)18(26)23-14-6-7-15-12(8-14)9-21-25-15/h2-9,17H,1H3,(H,21,25)(H,23,26)(H2,22,24,27)
InChI key
HEAIGWIZTYAQTC-UHFFFAOYSA-N
生化/生理作用
GSK180736A is a potent and selective dual inhibitor of a ROCK1 (Rho-associated, coiled-coil-containing protein kinase) and GRK2 (G protein-coupled receptor kinase 2). GSK180736A binds to the GRK2 active site. GSK180736A produces a significant cardiomyocytes contraction at 1 μM.
potent and selective dual inhibitor of a ROCK1 and GRK2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Kristoff T Homan et al.
ACS chemical biology, 10(1), 310-319 (2014-09-23)
Selective inhibitors of individual subfamilies of G protein-coupled receptor kinases (GRKs) would serve as useful chemical probes as well as leads for therapeutic applications ranging from heart failure to Parkinson's disease. To identify such inhibitors, differential scanning fluorimetry was used
Clark A Sehon et al.
Journal of medicinal chemistry, 51(21), 6631-6634 (2008-10-10)
Recent studies using known Rho-associated kinase isoform 1 (ROCK1) inhibitors along with cellular and molecular biology data have revealed a pivotal role of this enzyme in many aspects of cardiovascular function. Here we report a series of ROCK1 inhibitors which
Renee Bouley et al.
Molecular pharmacology, 92(6), 707-717 (2017-10-27)
G protein-coupled receptor kinases (GRKs) phosphorylate activated receptors to promote arrestin binding, decoupling from heterotrimeric G proteins, and internalization. GRK2 and GRK5 are overexpressed in the failing heart and thus have become therapeutic targets. Previously, we discovered two classes of
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