Revision 1

#9844Store at -20C

5.19 mg

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

3 Trask LaneDanversMassachusetts01923USA
For Research Use Only. Not for Use in Diagnostic Procedures.

Background

H-89 is a potent selective inhibitor of cAMP dependent protein kinase (PKA). The in vitro IC50 of H-89 for PKA is approximately 50 nM and in vivo the inhibitiory effect on PKA substrate phosphorylation and related cellular functions range from 10 μM to 30 μM (1,2). In addition to PKA, H-89 also exhibits a moderate inhibitory effect on PKG and PKCμ, with IC50 in the 500 nM range (1,3). The inhibitory effect of H-89 is due to its competitive binding to the ATP pocket on the kinase catalytic subunit (4).

  1. Chijiwa, T. et al. (1990) J Biol Chem 265, 5267-72.
  2. Meja, K.K. et al. (2004) J Pharmacol Exp Ther 309, 833-44.
  3. Johannes, F.J. et al. (1995) Eur J Biochem 227, 303-7.
  4. Engh, R.A. et al. (1996) J Biol Chem 271, 26157-64.

Molecular Formula

C20H20BrN3O2S • 2HCl

Molecular Weight

519.3 g/mol

Purity

>99%

CAS

127243-85-0

Solubility

Soluble in DMSO at 100mg/ml and EtOH at 2mg/ml.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

H-89 is supplied as 5.19 mg powder. Store at or below -20ºC. Before usage, dissolve powder in 0.5 ml DMSO to make 20 mM H-89. For working concentrations of 10 μM-20 μM, dilute DMSO stock 1:2000 to 1:1000. Treat cells with the desired concentration for 30 minutes.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

    Trademarks and Patents

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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