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Submit ReviewGo 6976 is a potent protein kinase C (PKC) inhibitor (IC50 = 7.9 nM). Discriminates between Ca2+-dependent and -independent isoforms of PKC in vitro; selectively inhibits PKCα and PKCβ1 (IC50 values are 2.3 and 6.2 nM respectively). Does not inhibit the activity of PKCδ, -ε, or -ζ (IC50 > 3μM). Also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC50 values are 5, 30, 130 and 370 nM respectively), PKCμ (PKD1) and the mitotic spindle checkpoint.
分子量 | 378.43 |
公式 | C24H18N4O |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 136194-77-9 |
PubChem ID | 3501 |
InChI Key | VWVYILCFSYNJHF-UHFFFAOYSA-N |
Smiles | O=C(NC3)C1=C3C(C4=CC=CC=C4N5CCC#N)=C5C2=C1C6=C(C=CC=C6)N2C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 3.78 | 10 |
以下数据基于产品分子量 378.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 26.42 mL | 132.12 mL | 264.25 mL |
0.5 mM | 5.28 mL | 26.42 mL | 52.85 mL |
1 mM | 2.64 mL | 13.21 mL | 26.42 mL |
5 mM | 0.53 mL | 2.64 mL | 5.28 mL |
参考文献是支持产品生物活性的出版物。
Martiny-Baron et al (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976 J.Biol.Chem. 268 9194 PMID: 8486620
Rennecke et al (1996) Immunological demonstration of protein kinase Cμ in murine tissues and various cell lines. Eur.J.Biochem. 242 428 PMID: 8973662
Behrens et al (1999) Go 6976 is a potent inhibitor of neurotrophin-receptor intrinsic tyrosine kinase. J.Neurochem. 72 919 PMID: 10037462
Grandage et al (2006) Go6976 is a potent inhibitor of JAK2 and FLT3 tyrosine kinases with significant activity in primary acute myeloid leukaemia cells. Br.J.Haematol. 135 303 PMID: 16956345
Stolz et al (2009) Pharmacologic abrogation of the mitotic spindle checkpoint by an indolocarbazole discovered by cellular screening efficiently kills cancer cells. Cancer Res. 69 3874 PMID: 19366805
If you know of a relevant reference for Go 6976, please let us know.
关键词: Go 6976, Go 6976 supplier, Potent, protein, kinases, C, inhibitors, inhibits, PKC, inhibitor, selective, alpha, beta1, isozymes, Go6976, Protein, Kinase, 2253, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Go 6976 的部分引用包括:
Buckles et al (2020) Rapid exposure of macrophages to drugs resolves four classes of effects on the leading edge sensory pseudopod: Non-perturbing, adaptive, disruptive, and activating PLoS One 15 PMID: 32469878
Shamseddine et al (2015) P53-dependent upregulation of neutral sphingomyelinase-2: role in doxorubicin-induced growth arrest. Cell Death Dis 6 e1947 PMID: 26512957
Yuan et al (2015) Inhibition of protein kinase C by isojacareubin suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo. Sci Rep 5 12889 PMID: 26245668
Yi et al (2014) Systematic analysis of bacterial effector-postsynaptic density 95/disc large/zonula occludens-1 (PDZ) domain interactions demonstrates Shigella OspE protein promotes protein kinase C activation via PDLIM proteins. J Neurosci 289 30101 PMID: 25124035
Farkas et al (2011) Identification of small molecule inhibitors of phosphatidylinositol 3-kinase and autophagy. J Biol Chem 286 38904 PMID: 21930714
Yeganeh et al (2019) Autophagy is required for lung development and morphogenesis. J Clin Invest 130 2904 PMID: 31162135
Lim and Joe (2013) A ROCK Inhibitor Blocks the Inhibitory Effect of Chondroitin Sulfate Proteoglycan on Morphological Changes of Mesenchymal Stromal/Stem Cells into Neuron-Like Cells. PLoS Biol 21 447 PMID: 24404335
Buchanan et al (2010) Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels. Neuron 68 948 PMID: 21145007
Muellner et al (2015) Targeting a cell state common to triple-negative breast cancers. J Biol Chem 11 789 PMID: 25699542
Yamamoto et al (2012) Raf kinase inhibitory protein is required for cerebellar long-term synaptic depression by mediating PKC-dependent MAPK activation. Biomol Ther (Seoul) 32 14254 PMID: 23055494
Schneberger et al (2018) Organic barn dust inhibits surfactant protein D production through protein kinase-c alpha dependent increase of GPR116. PLoS One 13 e0208597 PMID: 30543664
Lewis and Golsteyn (2016) Cancer cells that survive checkpoint adaptation contain micronuclei that harbor damaged DNA. Cell Cycle 15 3131 PMID: 27636097
Tam et al (2016) Tyrosine Binding Protein Sites Regulate the Intracellular Trafficking and Processing of Amyloid Precursor Protein through a Novel Lysosome-Directed Pathway. PLoS One 11 e0161445 PMID: 27776132
Shu et al (2014) Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals. PLoS One 9 e95259 PMID: 24748172
Lei et al (2017) PKC-α Triggers EGFR Ubiquitination, Endocytosis and ERK Activation in Podocytes Stimulated with High Glucose. Cell Physiol Biochem 42 281 PMID: 28535513
Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882
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