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CAS No.: 133053-19-7

Go 6983 Catalog No. CSN16527

Synonyms: Gö 6983;Goe 6983;GO-6983

Go6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively and less potent to PKCζ and inactive to PKCμ.

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PKCα

IC50:7nM PKCβ

IC50:7nM PKCγ

IC50:6nM PKCδ

IC50:10nM PKCζ

IC50:60nM
描述Protein kinase C (PKC) is a serine/threonine protein kinase, which plays a crucial role in signaling transduction mechanisms in many cell types and tissues. Gö 6983 is a pan-PKC inhibitor with IC50 values of 7nM, 7nM, 6nM, 10nM and 60nM (measure by protein kinase assay) for PKCα, PKCβ, PKCγ, PKCδ and PKCζ, whereas no activity against PKCμ with IC50 value of 20000nM. Gö 6983 is different with the normal pan-PKC inhibitor, such as staurosporine (IC50=40nM), for it has no effect on PKCμ, facilitating its ability to selective determination of PKCμ kinase activity in the presence of other PKC isoenzymes^[1]. Treatment with Gö6983 induced the surface expression of NCRs, including NCR1, NCR2 and NCR3 (measured by relative MFI ratio) in a time- and dose-dependent manner, in primary NK cells. Pre-treatment with Gö6983 for 4h enhanced NK cell-mediated tumor cell killing at an E:T ratio of 3:1, performing as increased apoptosis and cytotoxicity on HepG2, Hep3B and HeLa cells, but has no cytotoxicity itself. Injection with 22.0ug of Gö6983 once daily on days-2, 0, 2, and 4 strongly inhibited tumor metastasis in pulmonary tumor metastasis models^[2]. Inhibition of PKC through Gö 6983 could maintain ESC-specific epigenetic modifications at the chromatin domains of pluripotency genes and, thus maintain the expression of these genes in rat embryonic stem cells^[3]. It was found that Gö6983 could also inhibit the activity of PfPKB, a protein kinase B homologue in Plasmodium falciparum^[4].
作用机制Gö 6983 acts at the ATP binding site which is highly conserved across PKC isoforms. ^[5]
动物研究
剂量
Mice^[6] (i.p.): 2.5 mg/kg

给药途径
i.p.

动物研究
剂量	Mice^[6] (i.p.): 2.5 mg/kg
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2598 mL
- 11.2992 mL
- 22.5984 mL
- 5 mM
- 0.4520 mL
- 2.2598 mL
- 4.5197 mL
- 10 mM
- 0.2260 mL
- 1.1299 mL
- 2.2598 mL

技术信息

CAS号

133053-19-7

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26N4O3

运输

蓝冰

分子量

442.51

别名

Gö 6983;Goe 6983;GO-6983

溶解度

DMSO	100.0 mg/mL (226.0 mM)
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	2 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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靶点	Description	IC50
PKCα		IC50:7nM
PKCβ		IC50:7nM
PKCγ		IC50:6nM
PKCδ		IC50:10nM
PKCζ		IC50:60nM

Go 6983 Catalog No. CSN16527

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