BioProduct : Chemicals & Compounds : H 89,Protein kinase inhibitor H-89,H89,H 89

Product Name	H 89,Protein kinase inhibitor H-89,H89,H 89
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Product Description	H 89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM; weak inhibition on PKG, PKC, CK1, CK2 and others kinases. IC50 value: 48 nM [1] Target: PKA inhibitor in vitro: H-89 inhibits protein kinase A, in competitive fashion against ATP. To examine the role of protein kinase A in neurite outgrowth of PC12 cells, H-89 was applied along with nerve growth factor (NGF), forskolin, or dibutyryl cAMP. Pretreatment with H-89 led to a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells, and the NGF-induced protein phosphorylation was not not inhibited. H-89 also significantly inhibited the forskolin-induced neurite outgrowth from PC12D cells [1]. In intact single fibres of the flexor digitorum longus (FDB) muscle of the mouse, 1-3 microM H-89 had no noticeable effect on action-potential-mediated Ca2+ transients. Higher concentrations (4-10 microM) caused Ca2+ transient failure in fibres stimulated at 20 Hz in a manner indicative of action-potential failure. At 10-100 microM, H-89 also inhibited net Ca2+ uptake by the SR and affected the Ca2+-sensitivity of the contractile apparatus in rat skinned fibres [2]. in vivo: Intraperitoneal administration of H-89 (0.2 mg/100g) significantly increased seizure latency and threshold in PTZ-treated animals. Pretreatment of animals with PTX (50 and 100 mg/kg) attenuated the anticonvulsant effect of H-89 (0.2 mg/100g) in PTZ-exposed animals. H-89 (0.05, 0.2 mg/100g) prevented the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold [3].
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Price	$399/100mg
Specification	Numerous
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Vendor Information	MedChemExpress LLC  http://www.medchemexpress.com 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Middlesex County New Jersey 08852 United States Phone: 609-228-6898 Fax: 609-228-5909 E-Mail: sales@medchemexpress.com