Go 6983

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Chemical Structure| 133053-19-7 同义名 : Gö 6983;Goe 6983;Go6983 Go-6983
CAS号 : 133053-19-7
货号 : A199871
分子式 : C26H26N4O3
纯度 : 99%+
分子量 : 442.51
MDL号 : MFCD04040031
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(79.09 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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

生物活性
靶点

  • PKCβ

    PKCβ, IC50:7 nM

  • PKCγ

    PKCγ, IC50:6 nM

  • PKCζ

    PKCζ, IC50:60 nM

  • PKCα

    PKCα, IC50:7 nM

  • PKCδ

    PKCδ, IC50:10 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.30mL

2.26mL

1.13mL

22.60mL

4.52mL

2.26mL