HA-1004 dihydrochloride

Research use only, not for human use.

HA-1004 dihydrochloride?is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel proteinHA-1004, was shown to be a potent inhibitor of two cyclic nucleotide-dependent protein kinases, cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein kinase and the Ki values were 1.4 and 2.3 microM, respectively.?

HA-1004 dihydrochloride?is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel proteinHA-1004, was shown to be a potent inhibitor of two cyclic nucleotide-dependent protein kinases, cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein kinase and the Ki values were 1.4 and 2.3 microM, respectively.?HA-1004 relaxed rabbit aortic strips contracted by various agonists and with similar ED50 values.?Phenotolamine, propranolol and atropine did not affect this HA-1004-induced relaxation, thereby suggesting that this compound does not act through these membrane receptor associated mechanisms.?HA-1004 shifted the dose-response curve for CaCl2 to the right in a competitive manner in depolarized rabbit renal arterial strips.?This compound also relaxed the A-23187 and phenylephrine-induced contractions elicited in Ca++-free solution.?HA-1004 exerts its action at the intracellular or submembranal level.?This vasodilator has little effect on actomyosin adenosine triphosphatase and Ca++-calmodulin-dependent myosin light chain kinase.?Studies using its derivatives with various lengths of alkyl chain (C0-C6) indicated that the potencies of these compounds, as vasorelaxants, correlated well with their potential to inhibit cyclic nucleotide-dependent protein kinase.?HA-1004 should be a useful tool for investigating in smooth muscle, regulatory mechanism(s) by second messengers, cyclic AMP and cyclic GMP.

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Apoptosis

PKA

PKA|PKC|calcium channel

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92564-34-6

329.81

C12H16ClN5O2S

>98% (HPLC)

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C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCN=C(N)N.Cl

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(-20℃)

With Ice Pack

≥ 2 years