H 89 2HCl

CAT: 0013-GTR19163882-01Size: 1 gDry Ice: NoHazardous: No

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CAT#:0013-GTR19163882-01Size:1 g

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Description

H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. (In Vitro) :H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca2+ uptake by the SR and affectes the Ca2+-sensitivity of the contractile apparatus in rat skinned fibres. (In Vivo) :H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold.

CAS Number

130964-39-5

Product Name Alternative

5-Isoquinolinesulfonamide | Protein Kinase Inhibitor H-89

Purity

>98% (HPLC)

Solubility

DMSO:104 mg/mL (200.27 mM) ; Ethanol:<1 mg/mL (<1 mM) ; Water:6 mg/mL (11.55 mM)

Smiles

C1=CC2=C (C=CN=C2) C (=C1) S (=O) (=O) NCCNC/C=C/C3=CC=C (C=C3) Br.Cl.Cl

Molecular Formula

C20H20BrN3O2S.2HCl

Molecular Weight

519.28

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

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