371963-M

H-89, Dihydrochloride

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

• Szinonimák: 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
• Tapasztalati képlet (Hill-képlet): C₂₀H₂₀BrN₃O₂S · 2HCl
• CAS-szám: 127243-85-0
• Molekulatömeg: 519.28
• MDL-szám: MFCD00214119
• UNSPSC kód: 12352200

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥99% (HPLC)
• Forma: film (crystalline)
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze
• szín: clearoff-white
• oldhatóság: DMSO: 200 mg/mL; water: 25 mg/mL
• tárolási hőmérséklet: 2-8°C
• SMILES string: [S](=O)(=O)(NCCNC\C=C\c3ccc(cc3)Br)c1c2c(cncc2)ccc1
• 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+
• Nemzetközi kémiai azonosító kulcs: ZKZXNDJNWUTGDK-NSCUHMNNSA-N

Leírás

Általános leírás

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.

Biokémiai/fiziológiai hatások

Primary Target
PKA

Target K_i: 48 nM for protein kinase A

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

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

Egyéb megjegyzések

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.

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 1
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable