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  3. H-89, Dihydrochloride

H-89, Dihydrochloride #9844

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.
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Product Information

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).

Alternate Names

H89; inhibitor; PKA; PKCu; PKG

限制使用

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