| Identification | More | [Name]
H-8 DIHYDROCHLORIDE | [CAS]
113276-94-1 | [Synonyms]
H-8
H-8 HYDROCHLORIDE
H-8 DIHYDROCHLORIDE
H-8 dihydrochloride,98%
H8, dihydrochloride salt
H-8 dihydrochloride >98% (HPLC)
H-8 DIHYDROCHLORIDE POTENT INHIBITOR OF C
N-[2-(methylamino)ethyl]isoquinoline-5-sulfonamide
2-(5-isoquinolinylsulfonylamino)ethyl-methylammonium
N-[2-(METHYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE 2HCL
N-[2-(METHYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE, DI-HCL SALT
N-(2-[METHYLAMINO]ETHYL)-5-ISOQUINOLINESULFONAMIDE HYDROCHLORIDE
N-(2-(METHYLAMINO)ETHYL)ISOQUINOLINE-5-SULFONAMIDE DIHYDROCHLORIDE
N-[2-(METHYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE DIHYDROCHLORIDE
5-IsoquinolinesulfonaMide,N-[2-(MethylaMino)ethyl]-, hydrochloride (1:2) | [Molecular Formula]
C12H17Cl2N3O2S | [MDL Number]
MFCD00036962 | [Molecular Weight]
338.25 | [MOL File]
113276-94-1.mol |
| Chemical Properties | Back Directory | [Appearance]
white to off-white crystalline solid | [Melting point ]
221-222℃ (methanol water ) | [storage temp. ]
2-8°C
| [solubility ]
ethanol: 25 mg/mL, clear, colorless
| [form ]
Lyophilized | [color ]
White to Off-White | [Water Solubility ]
water: 10mg/mL | [InChI]
InChI=1S/C12H15N3O2S.2ClH/c1-13-7-8-15-18(16,17)12-4-2-3-10-9-14-6-5-11(10)12;;/h2-6,9,13,15H,7-8H2,1H3;2*1H | [InChIKey]
RJJLZYZEVNCZIW-UHFFFAOYSA-N | [SMILES]
C12=CC=NC=C1C=CC=C2S(=O)(=O)NCCNC.Cl.Cl | [CAS DataBase Reference]
113276-94-1(CAS DataBase Reference) |
| Safety Data | Back Directory | [Safety Statements ]
S22:Do not breathe dust .
S24/25:Avoid contact with skin and eyes . | [WGK Germany ]
3
| [HS Code ]
29334990 |
| Hazard Information | Back Directory | [Description]
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 | [Chemical Properties]
white to off-white crystalline solid | [Uses]
Active inhibitor of cyclic-nucleotide-dependent protein kinases. | [Biochem/physiol Actions]
cAMP and cGMP-dependent protein kinase inhibitor. | [storage]
Store at -20°C | [References]
[1] R A ENGH. 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.[J]. The Journal of Biological Chemistry, 1996, 271 42: 26157-26164. DOI: 10.1074/jbc.271.42.26157
[2] HIROYOSHI HIDAKA. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide-dependent protein kinase and protein kinase C[J]. Biochemistry Biochemistry, 1984, 23 21: 5036-5041. DOI: 10.1021/bi00316a032
[3] M HAGIWARA H H M Inagaki. Specific binding of a novel compound, N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide (H-8) to the active site of cAMP-dependent protein kinase.[J]. Molecular Pharmacology, 1987, 31 5: 523-528.
[4] P RICKERT E L J L Corden. Cyclin C/CDK8 and cyclin H/CDK7/p36 are biochemically distinct CTD kinases.[J]. Oncogene, 1999, 18 4: 1093-1102. DOI: 10.1038/sj.onc.1202399 |
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