Molecular structure of H-8 • 2HCl, CAS Number: 113276-94-1
H-8 • 2HCL (CAS 113276-94-1)
See product citations (3)
Alternate Names:
N-[2-(Methylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
Application:
H-8 • 2HCl is a selective inhibitor of PKA and cGKI
CAS Number:
113276-94-1
Purity:
≥98%%
Molecular Weight:
338.25
Molecular Formula:
C12H15N3O2S•2HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
H-8 • 2HCl inhibits PKA (IC50=1.2μM) and cGKI (IC50=0.48μM) selectively over PKC (IC50=15μM) and MLCK (IC50=68μM). Experiments suggest that this compound selectively targets cyclic nucleotide dependent protein kinases. Mechanistic studies show that H-8 • 2HCl blocks signaling pathways in cellular regulations. More detailed results show that H-8 binds cyclin-dependent kinases at a T-loop region in a competitive manner and prevents downstream RNA synthesis of genes. H-8 • 2HCl is an inhibitor of Cdk7, Cdk8, cyclin C and cyclin H.
H-8 • 2HCL (CAS 113276-94-1) References
- Forskolin modulation of desensitization at GABA(A) and glycine receptors is not mediated by cAMP-dependent protein kinase in isolated carp amacrine-like cells. | Li, P. and Yang, XL. 2001. Pflugers Arch. 441: 739-45. PMID: 11316256
- Mechanism of H-8 inhibition of cyclin-dependent kinase 9: study using inhibitor-immobilized matrices. | Shima, D., et al. 2003. Genes Cells. 8: 215-23. PMID: 12622719
- Leukotriene B4-induced human melanocyte pigmentation and leukotriene C4-induced human melanocyte growth are inhibited by different isoquinolinesulfonamides. | Morelli, JG., et al. 1992. J Invest Dermatol. 98: 55-8. PMID: 1309461
- Differentiation-linked activation of the respiratory burst in a monocytic cell line (U937) via Fc gamma RII. A study of activation pathways and their regulation. | Roberts, PJ., et al. 1991. J Immunol. 147: 3104-15. PMID: 1655905
- Differential growth inhibition of isoquinolinesulfonamides H-8 and H-7 towards multidrug-resistant P388 murine leukaemia cells. | Ido, M., et al. 1991. Br J Cancer. 64: 1103-7. PMID: 1684908
- Metabolic inhibitors and intermediate filament organization in human fibroblasts. | Klymkowsky, MW. 1988. Exp Cell Res. 174: 282-90. PMID: 3275545
- Phosphorylation of the guanine nucleotide exchange factor from rabbit reticulocytes regulates its activity in polypeptide chain initiation. | Dholakia, JN. and Wahba, AJ. 1988. Proc Natl Acad Sci U S A. 85: 51-4. PMID: 3422426
- Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. | Hidaka, H., et al. 1984. Biochemistry. 23: 5036-41. PMID: 6238627
- Cytokines increase neutral endopeptidase activity in lung fibroblasts. | Kondepudi, A. and Johnson, A. 1993. Am J Respir Cell Mol Biol. 8: 43-9. PMID: 8380249
- 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. | Engh, RA., et al. 1996. J Biol Chem. 271: 26157-64. PMID: 8824261
- Protein kinase modulation of GABAA currents in rabbit retinal rod bipolar cells. | Gillette, MA. and Dacheux, RF. 1996. J Neurophysiol. 76: 3070-86. PMID: 8930256
- A novel glutamate-mediated inhibitory mechanism linked with Ca2+/calmodulin-dependent protein kinase II in identified Euhadra neurons. | Watanabe, K., et al. 1997. J Neurobiol. 32: 139-49. PMID: 9032658
- Suppression of the nicotinic acetylcholine response in rat superior cervical ganglionic neurons by steroids. | Uki, M., et al. 1999. J Neurochem. 72: 808-14. PMID: 9930757
Inhibitor of:
Cdk7, Cdk8, cGKI, cyclin C, cyclin H, PKA, PKA Iα reg, PKC, and Ser/Thr Protein Kinase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
H-8 • 2HCL, 10 mg | sc-200526 | 10 mg | $60.00 | |||
H-8 • 2HCL, 50 mg | sc-200526A | 50 mg | $250.00 |