Biological Activity
Protein kinase A inhibitor that also inhibits several other kinases (IC50 values are 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b). Exhibits antinociceptive activity. Also available as part of the PKA TocrisetTM.
Compound Libraries
H 89 dihydrochloride is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox I and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 519.28 |
Formula | C20H20BrN3O2S.2HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 130964-39-5 |
PubChem ID | 5702541 |
InChI Key | GELOGQJVGPIKAM-WTVBWJGASA-N |
Smiles | O=S(C2=CC=CC1=CN=CC=C12)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.93 | 100 | |
water | 12.98 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 519.28. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.93 mL | 9.63 mL | 19.26 mL |
5 mM | 0.39 mL | 1.93 mL | 3.85 mL |
10 mM | 0.19 mL | 0.96 mL | 1.93 mL |
50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lochner and Moolman (2006) The many faces of H89: a review. Cardiovasc.Drug Rev. 24 261 PMID: 17214602
Yamada et al (2006) Involvement of cAMP response element-binding protein activation in salivary secretion. Pathobiology 73 1 PMID: 16785762
Vitolo et al (2002) Amyloid β-peptide inhibition of the PKA/CREB pathway and long-term potentiation: reversibility by drugs that enhance cAMP signaling. Proct.Natl.Acad.Sci.USA 99 13217 PMID: 12244210
Dolan and Nolan (2001) Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord. Neurosci.Lett. 309 157 PMID: 11514065
Keywords: H 89 dihydrochloride, supplier, Protein, kinases, A, inhibitors, inhibits, PKA, H89, dihydrochloride, Protein, Kinase, A, Protein, Kinase, A, Tocris Bioscience