Physical Appearance:  Off-white solid (m.p. 141-143°C)

Molecular Formula:  C₂₀H₂₀BrN₃O₂S·2HCl

Molecular Weight:  519.2

Purity:  ≥99% (HPLC)

Solubility:  Soluble in DMSO (25 mg/ml) and 50% ethanol/water (20 mg/ml)

Storage:  Store, as supplied, at 0-4°C for up to 1 year. Store solutions at -20°C for up to 4 months in DMSO.

Description:  A cell-permeable selective 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 μM) by blocking the action of Rho kinase II.

References:

1. T.Chijiwa et al. J.Biol.Chem. 1990 265 5267

2. M.Muroi and T.Suzuki Cell Signal 1993 5 289

3. M.Fujihara et al. J.Biol.Chem. 1993 268 14898

4. A.Azarani et al. J.Biol.Chem. 1995 270 23166

5. A.Azarani et al. J.Biol.Chem. 1995 270 20004

6. A.Azarani et al. J.Biol.Chem. 1995 270 17898

The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.