计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
GSK429286A, Rho 相关含线圈蛋白激酶 1 抑制剂；核糖体蛋白 S6 激酶 A1 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
GSK429286A是选择性的 ROCK1 抑制剂，IC50 值为14 nM。
Information
GSK429286A (RHO-15) is a selective inhibitor ofROCK1andROCK2withIC50of 14 nM and 63 nM, respectively.
In vitro
GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM. GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho.
In vivo
GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
英文别名
RHO-15 | N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
GSK429286A
生化机理
GSK429286A (RHO-15) 是 ROCK1 和 ROCK2 的选择性抑制剂，IC50 分别为 14 nM 和 63 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
Rho 相关含线圈蛋白激酶 1 抑制剂；核糖体蛋白 S6 激酶 A1 抑制剂
名称和识别符
EC号
689-442-9
分子类型
小分子
Isomeric SMILES
CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F
UN Number
Packing Group
III
分子量
432.37
Reaxy-Rn
10732416
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10732416&ln=
技术文档
高级数据
关联靶点（人）
ROCK1
Tclin
Rho 相关蛋白激酶 1(Rho-associated protein kinase 1)
(2 活性数据)
RPS6KA1
Tchem
核糖体蛋白 S6 激酶 α-1(Ribosomal protein S6 kinase alpha-1)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 48 mg/mL (198.09 mM); Ethanol: 48 mg/mL (198.09 mM); Water: Insoluble;
安全和危险性（GHS）
象形图
信号词
危险
危险声明
H301: 吞咽会中毒
预防措施声明
P321: 特殊处理（请参阅此标签上的...）。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P316: 如果吞咽：立即寻求紧急医疗救助。
WGK Germany
3
Class
6.1
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
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