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Merck
CN
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文件

365250

Sigma-Aldrich

Gö 6976

Gö 6976, CAS 136194-77-9, is a cell-permeable, reversible, and ATP-competitive inhibitor of PKC (IC₅₀ = 7.9 nM for rat brain). Exhibits selectively for PKCα (IC₅₀ = 2.3 nM) and βI (IC₅₀ = 6.2 nM).

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别名:
Gö 6976
经验公式（希尔记法）:
C24H18N4O
CAS号:
136194-77-9
分子量:
378.43
MDL编号:
MFCD00236434
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

检测方案

≥95% (HPLC)

形式

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

2-8°C

InChI

1S/C24H18N4O/c1-27-17-9-4-2-7-14(17)20-21-16(13-26-24(21)29)19-15-8-3-5-10-18(15)28(12-6-11-25)23(19)22(20)27/h2-5,7-10H,6,12-13H2,1H3,(H,26,29)

InChI key

VWVYILCFSYNJHF-UHFFFAOYSA-N

一般描述

一种细胞可渗透性、可逆和ATP竞争性的蛋白激酶C（PKC；大鼠脑的IC50=7.9 nM）抑制剂。选择性抑制Ca2+依赖性PKCα-同工酶（IC50=2.3 nM）和PKCβI（IC50=6.2 nM）。即使在微摩尔水平下，也不会影响不依赖Ca2+的PKCδ-，ε-和ζ-同工酶的激酶活性。据报道，在较高浓度（IC50=20 nM）下可抑制PKCµ。也可获得500 µg/mL的Gö 6976（目录编号365253）在无水DMSO中的溶液。
一种细胞可渗透性、可逆和ATP竞争性的蛋白激酶C（PKC；大鼠脑的IC50=7.9 nM）抑制剂。选择性抑制Ca2+依赖性PKCα-同工酶（IC50=2.3 nM）和PKCβI（IC50=6.2 nM）。即使在微摩尔水平下，也不会影响不依赖Ca2+的PKCδ-，ε-和ζ-同工酶的激酶活性。艾滋病病毒I型诱导的强效拮抗剂。

生化/生理作用

主要靶标
PKC
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：7.9 nM，针对大鼠脑PKC；针对Ca2+依赖性PKCα-同工酶和PKCβI分别为2.3 nM和6.2 nM

警告

毒性：标准处理（A）

重悬

复溶后，等分并冷冻保存（-20°C）。储备液可在-20°C最长稳定4个月。

其他说明

Gschwendt, M., et al. 1996.FEBS Lett.392, 77.
Wenzel-Seifert, K., et al. 1994.Biochem.Biophys.Res. Commun.200, 1536.
Martiny-Baron, G.M., et al. 1993.J. Biol. Chem.268, 9194.
Qatsha, K.A., et al. 1993.Proc.Natl.Acad.Sci. USA90, 4674.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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