H-89 Inhibitor CAS No. 127243-85-0

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KI0575	H-89	1 mg	$126.72

Chemical Characteristic

Product Name	H-89
CAS No.	127243-85-0
Molecular Weight	446.36
Formula	C₂₀H₂₀BrN₃O₂S
Chemical Name	N-[2-[[3-(4-Bromophenyl)-2-propen-1-yl]amino]ethyl]-5-isoquinolinesulfonamide
Smiles	c1nccc2c(cccc12)S(=O)(=O)NCCNC/C=C/c1ccc(cc1)Br
Chemical Structure

Biological activities

H-89 is a specific cyclic AMP-dependent protein kinase A (protein kinase A) inhibitor. H-89 inhibits protein kinase A (PKA), PKB, PKG and PKC kinases with IC50 of 0.04, 2.5, 0.88 and 15 μM, respectively.^[1] H-89 has a potent and selective inhibitory action against PKA, with a Ki of 48 nM. H-89 inhibits these kinases, including PKG, PKC, casein kinase I and II, myosin light chain kinase, and Ca²⁺/calmodulin-dependent protein kinase II with Ki of 0.48, 31.7, 38.3, 136.7, 28.3, and 29.7 μM, respectively. H-89 also significantly inhibits the forskolin-induced neurite outgrowth from PCl2D cells. Pretreatment of PCl2D cells with H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in cell lysates. ^[2] Pretreatment with H-89 significantly attenuates isoproterenol-stimulated cAMP accumulation. H-89 acts as a beta-2 AR antagonist of surprisingly high affinity with a Ki of 0.18 μM. H-89 inhibits [³H]dihydroalprenolol to both beta-2 AR and beta-1 AR with Ki of 0.24 and 0.50 μM, respectively. ^[3] H-89 decreases Kv1.3 currents and accelerates the decay rate of current inactivation in a concentration- dependent manner with an IC50 of 1.70 μM. ^[4]

Protocols

H-89 is dissolved in DMSO. ^[4]

References

[1] Reuveni H, et al. Toward a PKB inhibitor: modification of a selective PKA inhibitor by rational design. Biochemistry. 2002, 41(32): 10304-10314. [2] Chijiwa T, et al. Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H- 89), of PC12D pheochromocytoma cells. J Biol Chem. 1990, 265(9): 5267-5272. [3] Penn RB, et al. Pharmacological inhibition of protein kinases in intact cells: antagonism of beta adrenergic receptor ligand binding by H-89 reveals limitations of usefulness. J Pharmacol Exp Ther. 1999, 288(2): 428-437. [4] Choi J, et al. Inhibition of Kv1.3 channels by H-89 (N-[2- (p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) independent of protein kinase A. Biochem Pharmacol. 2001, 61(8): 1029-1032.

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