HA-1077 dihydrochloride has been shown to be a vasodilating agent as well as a potent inhibitor of Rock-2 (Rho-associated Kinase II), cGKI (cGMP-dependent protein kinase), PKA (cAMP-dependent protein kinase), MYLK, and CaMKII. Rho kinase signaling pathways are thought to cause invasion, migration, and proliferation of certain cells. Studies have shown this compound can also inhibit myosin light chain kinase in vitro and suppress cell rounding by myosin light chain phosphorylation. Mechanistic experiments report that HA-1077 inhibits vascular smooth muscle contraction by acting as a calcium channel protein inhibitor. HA-1077 dihydrochloride is an inhibitor of MSK1, PKC, PRK2 and Rsk-2.
1. Asano, T., et al. 1987. J. Pharmacol. Exp. Ther. 241: 1033-1040. PMID: 3598899 2. Asano, T., et al. 1989. Br. J. Pharmacol. 98: 1091-1100. PMID: 2611484 3. Sasaki, Y., et al. 1990. Biochem. Biophys. Res. Commun. 171: 1182-1187. PMID: 2222437 4. Nagumo, H., et al. 2000. Am. J. Physiol., Cell Physiol. 278: C57-C65. PMID: 10644512
Soluble in water (>20 mg/ml), DMSO (~2 mg/ml), methanol, DMF (~2 mg/ml), and PBS, pH 7.2 (~5 mg/ml).
Store at -20° C
agonist-induced activation of NADPH oxidase: IC50 = 15 µM (human neutrophils); Rho-associated Kinase II (ROCK-II): IC50 = 1.9 µM; Protein Kinase C-related Kinase 2 (PRK2): IC50 = 4 µM; Mitogen- and Stress-Activated Protein Kinase (MSK1): IC50 = 5 µM; Mitogen Activated Protein Kinase-Activated Protein Kinase 1b (MAPKAP-K1b): IC50 = 15 µM
Rho kinase: Ki= 0.33 µM; protein kinase A: Ki= 1.6 µM; protein kinase G: Ki= 1.6 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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TaoTao, X. et al. (PubMed 26245530) reported that the Rho-kinase inhibitor HA-1077 reduces allergic airway inflammation and mucus hypersecretion by regulating STAT6 and NF B. -SCBT Publication Review
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