| 货号 | 10010249-5mg |
| 描述 | The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.1,2,3 H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC50 values of 47 and 6.2 µM, respectively.4 |
| 别名 | Protein Kinase Inhibitor H-8; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Engh, R.A.,Girod, A.,Kinzel, V., et al. Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89 structural implications for selectivity. The Journal of Biological Chemisty 271(42), 26157-26164 (1996). 2.Hidaka, H.,Inagaki, M.,Kawamoto, S., et al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry 23, 5036-5041 (1984). 3.Hagiwara, M.,Inagaki, M., and Hidaka, H. Specific binding of a novel compound, N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide (H-8) to the active site of cAMP-dependent protein kinase. Molecular Pharmacology 31, 523-528 (1987). 4.Rickert, P.,Corden, J.L., and Lees, E. Cyclin C/CDK8 and cyclin H/CDK7/p36 are biochemically distinct CTD kinases. Oncogene 18, 1093-1102 (1999). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 338.3 |
| 分子式 | C12H15N3O2S • 2HCl |
| CAS号 | 113276-94-1 |
| 稳定性 | ≥ 2 years |
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