H-8 dot 2HCLA selective inhibitor of PKA and cGKI

H-8 • 2HCL (CAS 113276-94-1)

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Synonym: N-[2-(Methylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
Application: A selective inhibitor of PKA and cGKI
CAS Number: 113276-94-1
Purity: ≥98%%
Molecular Weight: 338.25
Molecular Formula: C12H15N3O2S•2HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

1. Hidaka, H., et al. 1984. Biochemistry. 23: 5036-5041. PMID: 6238627
2. Ido, M., et al. 1991. Br. J. Cancer. 64: 1103-1107. PMID: 1684908
3. Engh, R.A., et al. 1996. J. Biol. Chem. 271: 26157-26164. PMID: 8824261
4. Shima, D., et al. 2003. Genes Cells. 8: 215-223. PMID: 12622719

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), 1:1 ethanol/water (25 mg/ml), methanol, and water.
Storage :
Store at -20° C
Refractive Index :
n20D 1.61
IC50 :
PKA: IC50 = 1.2 µM; PKG: IC50 = 0.48 µM; PKC: IC50 = 15 µM; MLCK: IC50 = 68 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
150584
SMILES :
CNCCNS(=O)(=O)C1=CC=CC2=C1C=CN=C2.Cl.Cl

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Certificate of Analysis

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H-8 dot 2HCL  Product Citations

See how others have used H-8 dot 2HCL. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 9841737  Light, DB. et al. 1998. J. Membr. Biol. 166: 119-132.

PMID: # 3574296  Hagiwara, M. et al. 1987. Mol. Pharmacol. 31: 523-528.

Citations 1 to 2 of 2 total
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