371963-M

H-89, Dihydrochloride

A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (K_i = 48 nM).

• Sinonimo/i: H-89, Dihydrochloride, N-[2-(( p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III, N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III
• Formula empirica (notazione di Hill): C₂₀H₂₀BrN₃O₂S · 2HCl
• Numero CAS: 127243-85-0
• Peso molecolare: 519.28
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥99% (HPLC)
• Forma fisica: film (crystalline)
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: clearoff-white
• Solubilità: DMSO: 200 mg/mL; water: 25 mg/mL
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C20H20BrN3O2S/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20/h1-10,12,15,22,24H,11,13-14H2/b3-2+; ZKZXNDJNWUTGDK-NSCUHMNNSA-N

Descrizione

Descrizione generale

A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (K_i = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (K_i = 28.3 µM), Ca²⁺/calmodulin-dependent protein kinase II (K_i = 29.7 µM), protein kinase C (K_i = 31.7 µM), casein kinase I (K_i = 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.

A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (K_i = 48 nM). Inhibits other kinases only at much higher concentrations: CaM kinase II (K_i = 29.7 µM), casein kinase I (K_i = 38.3 µM), myosin light chain kinase (K_i = 28.3 µM), protein kinase C (K_i = 31.7 µM), and ROCK-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, GEFII, or Epac (exchange protein directly activated by cAMP). Enhances radiation-induced apoptosis in the human cell line BM 13674. A 10 mM (1 mg/193 µl) solution of H-89, 2HCl (Cat. No. 371962) in DMSO is also available.

Azioni biochim/fisiol

Primary Target
PKA

Target K_i: 48 nM for protein kinase A

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, store in the refrigerator (4°C). Stock solutions are stable for at up to 4 months at 4°C.

Altre note

Leemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther.300, 1000.
Davies, S.P., et al. 2000. Biochem. J.351, 95.
Kawasaki, H., et al. 1998. Science 282, 2275.
de Rooij, J., et al. 1998. Nature 396, 474.
Findik, D., et al. 1995. J. Cell. Biochem.57, 12.
Geilen, C.C. 1992. FEBS Lett.309, 381.
Chijiwa, T., et al. 1990. J. Biol. Chem.265, 5267.
Combest, W.L., et al. 1988. J. Neurochem.51, 1581.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable