| Identification | More | [Name]
H-89 dihydrochloride | [CAS]
127243-85-0 | [Synonyms]
H-89
H-89 DIHYDROCHLORIDE
H-89 HYDROCHLORIDE
N-[2-(P-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINE SULFONAMIDE
N-[2-(P-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE 2HCL
N-[2-(P-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINE SULFONAMIDE, DIHYDROCHLORIDE
N-(2-[P-BROMOCINNAMYLAMINO]ETHYL)-5-ISOQUINOLINESULFONAMIDE HYDROCHLORIDE
N-[2-[P-BROMOCINNAMYLAMINO]-ETHYL]-5-ISOQUINOLINESULFONMIDE | [Molecular Formula]
C20H20BrN3O2S | [MDL Number]
MFCD00214119 | [Molecular Weight]
446.36 | [MOL File]
127243-85-0.mol |
| Chemical Properties | Back Directory | [Appearance]
White Solid | [Melting point ]
195-200°C | [Boiling point ]
639.7±65.0 °C(Predicted) | [density ]
1.436 | [storage temp. ]
2-8°C
| [solubility ]
H2O: ≥10 mg/mL
| [form ]
powder
| [pka]
10.43±0.50(Predicted) | [color ]
off-white
| [Usage]
Selective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of
0.0048 uM | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. | [CAS DataBase Reference]
127243-85-0(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 ]
29350090 |
| Hazard Information | Back Directory | [Description]
H-89 (127243-85-0) is a commonly used inhibitor of protein kinase A (PKA? IC50?= 140 nM).? Inhibits a variety of other kinases including S6K1 (IC50?= 80 nM), MSK1 (120 nM), ROCK II (270 nM), PKBα (2.6 μM), PKD, PRK2, RSK1 and 2, SGK, AMPK, CHK1 and MAPKAP-K1b (2.8 μM).1,2 | [Chemical Properties]
White Solid | [Uses]
Selective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of
0.0048 uM | [Uses]
Selective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of 0.0048 uM. | [Definition]
ChEBI: A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N1-[3-(4-bromophenyl)prop-2-en-1-yl]et
ane-1,2-diamine. | [General Description]
A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (Ki = 28.3 μM), Ca2+/calmodulin-dependent protein kinase II (Ki = 29.7 μM), protein kinase C (Ki = 31.7 μM), casein kinase I (Ki = 38.3 μM), and Rho Kinase II (IC50 = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs), such as GEFI or Epac (exchange protein directly activated by cAMP) and GEFII. Reported to induce neurite formation in NG 108-15 cells (~1 mM) by blocking the action of Rho kinase II. | [Biological Activity]
Protein kinase A inhibitor that also inhibits several other kinases (IC 50 values are 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKB α and MAPKAP-K1b). | [Biochem/physiol Actions]
Target Ki: 48 nM for protein kinase A | [storage]
Store at -20°C | [References]
1) Lochner and Moolman (2006),?The many faces of H89: a review; Cardiovasc. Drugs,?24?261
2) Bain?et al. (2007),?The selectivity of protein kinase inhibitors: a further update; Biochem.J.?408(Pt3)?297 |
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