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CAS No.: 136194-77-9

Go6976 Catalog No. CSN16571

Synonyms: PD406976;Gö 6976;GO-6976

Gö6976 is a pan inhibitor of Ca²⁺-dependent PKC isozymes, PKCα and PKCβ1, with IC50 values of 2.3nM and 6.2nM, respectively, but has no effect on Ca²⁺-independent PKC isozymes PKCδ, ε and ζ.

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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 PKCβ1

IC50:6.2nM PKCα

IC50:2.3nM PKC (rat brain)

IC50:7.9nM
描述PKC (Protein kinase C) is a ubiquitous phospholipid-dependent protein kinase which plays a crucial role in signaling transduction related to neuronal function, cell growth and differentiation, cell motility, secretion and cellular metabolism and smooth muscle contraction. Gö6976 is a pan inhibitor of Ca²⁺-dependent PKC isozymes, PKCα and PKCβ1, with IC50 values of 2.3nM and 6.2nM, respectively, but has no effect on Ca²⁺-independent PKC isozymes PKCδ, ε and ζ (measured by enzymatic activities of different PKC isozymes). This facilitates its ability to discriminate between Ca²⁺-dependent and -independent isoforms of PKC in vitro. Incubation with Gö6976 1μM for 72h can induce 90% apoptosis in NB4 cells and complete loss of full-length caspase 3. Meanwhile, caspase 8 can be seen in NB4 cells treated with 10μM Gö6976 for 8h. For Gö6976 is a multiple target inhibitor, it also inhibits JAK2/3 tyrosine kinases, PKCμ, as well as mitotic spindle checkpoint. Gö6976 could reduce the JAK2 auto-kinase activity and JAK3 kinase activity at concentration of 1μM in an in vitro kinase assay. Consistent with this, pre-incubation with Gö6976 could reduce IL2-stimulated phosphorylation of STAT5, the JAK3 dependent signaling, in a dose-dependent manner in peripheral blood-derived lymphocytes incubated with 10mg/ml PHA for 72h. It was reported that the enzyme activity of PKCμ is effectively suppressed by Gö6976 but not by Gö 6983. Gö6976 treatment can potently override a spindle checkpoint–mediated mitotic arrest by abrogating the phosphorylation and kinetochore localization of several spindle checkpoint proteins and cause severe mitotic abnormalities and chromosome alignment defects, which are not properly detected by the drug-inactivated spindle checkpoint.
作用机制Gö6976 is an ATP-competitive inhibitor.
动物研究
剂量
Monkey: 2 mg/kg(i.v.)
Mice (i.p): 2.5 mg/kg

给药途径
i.v., i.p.

动物研究
剂量	Monkey: 2 mg/kg(i.v.) Mice (i.p): 2.5 mg/kg
给药途径	i.v., 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
- 2.6425 mL
- 13.2125 mL
- 26.4250 mL
- 5 mM
- 0.5285 mL
- 2.6425 mL
- 5.2850 mL
- 10 mM
- 0.2642 mL
- 1.3212 mL
- 2.6425 mL

技术信息

CAS号	136194-77-9	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C24H18N4O	运输	蓝冰
分子量	378.43	别名	PD406976;Gö 6976;GO-6976

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靶点	Description	IC50
PKCβ1		IC50:6.2nM
PKCα		IC50:2.3nM
PKC (rat brain)		IC50:7.9nM

Go6976 Catalog No. CSN16571

靶点选择性

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