Molecular Formula | C20H20BrN3O2S |
Molar Mass | 446.36 |
Density | 1.436 |
Melting Point | 195-200°C |
Boling Point | 639.7±65.0 °C(Predicted) |
Flash Point | 361.8°C |
Solubility | H2O: ≥10mg/mL |
Vapor Presure | 1.95E-18mmHg at 25°C |
Appearance | White-like powder |
Color | off-white |
pKa | 10.43±0.50(Predicted) |
Storage Condition | 2-8°C |
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. |
MDL | MFCD00214120 |
Physical and Chemical Properties | Solubility: H2O: ≥ 10 mg/mL storage condition: 2-8 ℃ WGK Germany:3 |
In vitro study | H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca 2+ uptake by the SR and affectes the Ca 32 -sensitivity of the contractile apparatus in rat skinned fibres. |
In vivo study | H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
HS Code | 29350090 |
biological activity | H-89 is an effective and selective cAMP-dependent protein kinase A inhibitor with an IC50 value of 48 nM, and its inhibitory effect on PKG,PKC,Casein Kinase and other kinases is very weak. |
target | IC50: 48 nM (protein kinase A) |