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HA-1004 dihydrochloride

Catalog No. T8681   CAS 92564-34-6

HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein

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HA-1004 dihydrochloride Chemical Structure
HA-1004 dihydrochloride, CAS 92564-34-6
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Description HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
In vivo HA-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[1].
Molecular Weight 329.81
Formula C12H16ClN5O2S
CAS No. 92564-34-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

TargetMolReferences and Literature

1. Ishikawa T , Inagaki M , Watanabe M , et al. Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase[J]. Journal of Pharmacology and Experimental Therapeutics, 1985, 235(2):495-499. 2. Maurice G H , Ruey T L , Chipkin S R . The isoquinoline sulfonamide inhibitors of protein phosphorylation, H-7, H-8, and HA-1004, also inhibit RNA synthesis: studies on responses of adipose tissue to growth hormone.[J]. Endocrinology, 1990(1):441.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Calcium Antagonist Library

Related Products

Related compounds with same targets
PKC-theta inhibitor PKC-theta inhibitor 1 Cycloheterophyllin DCP-LA SAMβA TFA AJH-836 HIV-1 protease-IN-10 PKCβII Peptide Inhibitor I

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Keywords

HA-1004 dihydrochloride 92564-34-6 Chromatin/Epigenetic Cytoskeletal Signaling Membrane transporter/Ion channel Metabolism Tyrosine Kinase/Adaptors PKC PKA Calcium Channel HA1004 Dihydrochloride HA 1004 HA 1004 Dihydrochloride HA1004 HA-1004 Dihydrochloride HA 1004 dihydrochloride HA-1004 HA1004 dihydrochloride inhibitor inhibit

 

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