SML2296
GSK180736A
≥98% (HPLC)
别名:
4-(4-Fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-5-pyrimidinecarboxamide, GSK 180736A
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关于此项目
经验公式（希尔记法）:
C19H16FN5O2
化学文摘社编号:
分子量:
365.36
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
产品名称
GSK180736A, ≥98% (HPLC)
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
SMILES string
O=C(NC1=CC=C(NN=C2)C2=C1)C3=C(C)NC(NC3C4=CC=C(F)C=C4)=O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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
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
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