HA-1004 

HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models^[1][2][3].

cyclic GMP-dependent protein kinase, cyclic AMP-dependent protein^[2]

HA-1004 (40 nmol/day; infused by minipumps and delivered at 1 μL/h), it acts simultaneously with morphine to antagonize the phosphorylation of ERK1/2 and TH and inhibit the increase of NA conversion during morphine withdrawal in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

293.34

C₁₂H₁₅N₅O₂S

91742-10-8

Solid

White to off-white

O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC(N)=N)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Almela P, et al. Crosstalk between G protein-coupled receptors (GPCRs) and tyrosine kinase receptor (TXR) in the heart after morphine withdrawal. Front Pharmacol. 2013 Dec 27;4:164.  [Content Brief]

  [2]. Goodman HM, et al. 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. Endocrinology. 1990 Jan;126(1):441-50.  [Content Brief]

  [3]. Ishikawa T, et al. Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase. J Pharmacol Exp Ther. 1985 Nov;235(2):495-9.  [Content Brief]