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9844
H-89, Dihydrochloride
Activators & Inhibitors
Chemical Modulators

H-89, Dihydrochloride #9844

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H-89, Dihydrochloride: Image 1

Structure of H-89

H-89, Dihydrochloride: Image 2

Western blot analysis of extracts from SKNMC cells, untreated or treated with indicated concentrations of H-89 for 30 minutes, followed by stimulation with 30 µM Forskolin for 10 minutes. The phosphorylation of CREB was detected using Phospho-CREB (Ser133) (87G3) Rabbit mAb #9198 (upper), CREB (48H2) Rabbit mAb #9197 was used as a loading control (lower). H-89 inhibition of Forskolin induced PKA phosphorylation on CREB at Ser133 is shown.

Product Usage Information

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.

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.

Product Description

Molecular Weight 519.3 g/mol
Purity

>99%

Molecular Formula

C20H20BrN3O2S • 2HCl

CAS 127243-85-0
Solubility Soluble in DMSO at 100mg/ml and EtOH at 2mg/ml.

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.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 9844S
Product # Size Price
9844S
5.19 mg $ 118