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Submit ReviewH-7 dihydrochloride is a protein kinase inhibitor (IC50 values for inhibition of PKA, PKG, PKC and myosin light chain kinase are 3.0, 5.8, 6.0 and 97.0 μM, respectively. H-7 shows antiviral activity against influenza A (IC50 = 10 μM) in vitro. H-7 also inhibits interleukin-stimulated secretion of IgM and blocks PMA-stimulated interleukin 1β production.
H-7 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 364.29 |
公式 | C14H17N3O2S.2HCl |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 108930-17-2 |
PubChem ID | 73332 |
InChI Key | OARGPFMFRLLKPF-UHFFFAOYSA-N |
Smiles | Cl.Cl.CC1CNCCN1S(=O)(=O)C1=CC=CC2=CN=CC=C12 |
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 | |||
water | 36.43 | 100 | |
DMSO | 7.29 | 20 |
以下数据基于产品分子量 364.29。 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 |
---|---|---|---|
1 mM | 2.75 mL | 13.73 mL | 27.45 mL |
5 mM | 0.55 mL | 2.75 mL | 5.49 mL |
10 mM | 0.27 mL | 1.37 mL | 2.75 mL |
50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Hidaka et al (1984) Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry 23 5036 PMID: 6238627
Quick et al (1992) The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source. Biochem.Biophys.Res.Commun. 187 657 PMID: 1530632
Ratz et al (1990) Effect of the kinase inhibitor, H-7, on stress, crossbridge phosphorylation, muscle shortening and inositol phosphate production in rabbit arteries. J.Pharmacol.Exp.Ther. 252 253 PMID: 2299593
Kurokawa et al (1990) Inhibitory effect of protein kinase C inhibitor on the replication of influenza type A virus. J.Gen.Virol. 71 2149 PMID: 1698925
Hurme et al (1990) Control of interleukin-1 beta expression by protein kinase C and cyclic adenosine monophosphate in myeloid leukemia cells Blood 76 2198 PMID: 2175219
If you know of a relevant reference for H-7 dihydrochloride, please let us know.
关键词: H-7 dihydrochloride, H-7 dihydrochloride supplier, Protein, kinase, Broad, Spectrum, inhibitors, inhibits, H7, dihydrochloride, Kinase, Inhibitors, Influenza, Viruses, 0542, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 H-7 dihydrochloride 的部分引用包括:
Barcomb et al (2013) Enzymatic activity of CaMKII is not required for its interaction with the glutamate receptor subunit GluN2B. Front Mol Neurosci 84 834 PMID: 24056996
Ludgate et al (2012) Cyclin-dependent kinase 2 phosphorylates s/t-p sites in the hepadnavirus core protein C-terminal domain and is incorporated into viral capsids. J Virol 86 12237 PMID: 22951823
Zhao et al (2018) TRPV4 Blockade Preserves the Blood-Brain Barrier by Inhibiting Stress Fiber Formation in a Rat Model of Intracerebral Hemorrhage. Front Mol Neurosci 11 97 PMID: 29636662
Belmeguenai and Hansel (2005) A role for protein phosphatases 1, 2A, and 2B in cerebellar long-term potentiation. Mol Pharmacol 25 10768 PMID: 16291950
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H7 was studied for its inhibitory role in cAMP dependent protein kinase with ICso values of 18 and 16 gM respectively.
Cultures were incubated for 16 hours at 37 ~ in an atmosphere of 5% CO2 and 95% humidified air. 1~tCi of [3H]-thymidine was added to each well and cultures incubated for a further 5 hours. Cells were then harvested onto glass fibre filters, washed and incorporated radioactivity determined by liq- uid scintillation spectrometry.