Go 6976
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Go 6976是一种选择性的PKC抑制剂,IC50值为20 nM[1][2].
蛋白激酶C(PKC)属于蛋白激酶家族,通过对丝氨酸和苏氨酸残基上羟基的磷酸化作用,在控制其他蛋白功能中起着重要作用[1-3].
Go 6976是一种有效的PKC抑制剂,而且比已报道的PKC抑制剂H-7活性更强.当对nRT细胞测试时,Go 6976通过抑制Ca2+依赖性PKC通路,以10 μM的浓度明显减少了约40%的基线T-电流振幅[3].在HIV-1感染的T细胞系ACH-2和U1中,用Go 6976处理可有效地阻断Bryostain 1或肿瘤坏死因子α诱导的病毒转录,从而抑制细胞内病毒蛋白合成和病毒脱落,也可以阻断IL-6介导的转录后病毒蛋白诱导[2].
也有报道,Go 6976是一种有效的EGFR和FLT3抑制剂,IC50值范围分别是0.033 nM~3.3 μM和0.7 nM[4][5].
参考文献：
[1]. Gschwendt, M., et al., Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett, 1996. 392(2): p. 77-80.
[2]. Qatsha, K.A., et al., Go 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low-level-producing reservoir cells in vitro. Proc Natl Acad Sci U S A, 1993. 90(10): p. 4674-8.
[3]. Joksovic, P.M., et al., Mechanisms of inhibition of T-type calcium current in the reticular thalamic neurons by 1-octanol: implication of the protein kinase C pathway. Mol Pharmacol, 2010. 77(1): p. 87-94.
[4]. Taube, E., et al., A novel treatment strategy for EGFR mutant NSCLC with T790M-mediated acquired resistance. Int J Cancer, 2012. 131(4): p. 970-9.
[5]. Yoshida, A., et al., Go6976, a FLT3 kinase inhibitor, exerts potent cytotoxic activity against acute leukemia via inhibition of survivin and MCL-1. Biochem Pharmacol, 2014. 90(1): p. 16-24.
| Physical Appearance | A crystalline solid |
| Storage | Desiccate at -20°C |
| M.Wt | 378.43 |
| Cas No. | 136194-77-9 |
| Formula | C24H18N4O |
| Synonyms | Go6976; Go-6976 |
| Solubility | ≥15.77 mg/mL in DMSO |
| Chemical Name | 3-(13-methyl-5-oxo-6,7-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12(13H)-yl)propanenitrile |
| SDF | Download SDF |
| Canonical SMILES | O=C1NCC2=C3C(N(CCC#N)C4=CC=CC=C34)=C5N(C)C6=CC=CC=C6C5=C21 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
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细胞系 |
HEL细胞 |
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溶解方法 |
在DMSO中的溶解度大于10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
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反应条件 |
4 h，1 μM |
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应用 |
Go 6976是一个选择性的蛋白激酶C（PKC）钙依赖性同功酶的抑制剂，在体外对JAK2具有直接有效的抑制作用。Go 6976也可以抑制表达TEL-JAK2融合蛋白的细胞中的信号转导、增殖和存活。使用Go 6976处理原发性急性髓性白血病细胞可减少STAT的磷酸化和组成型STAT活性。 |
| 动物实验[2]: | |
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动物模型 |
6-8周龄的Balb/c小鼠 |
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剂量 |
2.5 mg/kg，腹腔注射 |
|
应用 |
Go 6976显著抑制LPS诱导的蛋白激酶D激活，减轻LPS/D-GalN诱导的肝损伤，提高LPS/D-GalN给药小鼠的存活率。Go 6976也能够抑制小鼠肝中丝裂原活化蛋白激酶（MAPKs）的激活，减少肿瘤坏死因子ɑ（TNF-ɑ）的表达，减少细胞凋亡和髓过氧化物酶（MPO）的活性 |
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注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
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References: [1]. Grandage V L, Everington T, Linch D C, et al. Go 6976 is a potent inhibitor of the JAK 2 and FLT3 tyrosine kinases with significant activity in primary acute myeloid leukaemia cells[J]. British journal of haematology, 2006, 135(3): 303-316. [2]. Duan G J, Zhu J, Xu C Y, et al. Protective effect of Go 6976, a PKD inhibitor, on LPS/d-GalN-induced acute liver injury in mice[J]. Inflammation research, 2011, 60(4): 357-366. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
