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HA-1077, fasudil, 5 mg  

HA-1077, fasudil, 5 mg

1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine dihydrochloride

Synonyms: HA1077, fasudil
inhibitor of ROCKII, Rho kinase, PRK2 and MSK1, also inhibits PKA, PKG, S6K1 and MAPKAP-K1b, MLCK and CaMKII

More details

PKI-HA1077-005

Availability: on stock

80,00 €

Background: Inhibitor of ROCKII, Rho kinase, PRK2 and MSK1, also inhibits PKA, PKG, S6K1 and MAPKAP-K1b, myosin light chain kinase (MLCK) and Ca2+/calmodulin dependent protein kinase II (CaMKII). Cell permeable Ca2+ antagonist with antivasospastic properties.

Chemical formula: C14H17N3O2S . 2HCl
Molecular weight: 291.4 + 73.0 g/mol
Purity: >98%
Form: solid
Solubility: soluble in water
CAS number: 103745-39-7

Also available predissolved at 10 mM in our kinase inhibitor Set (AGC group).

Product specific literature references:

Asano T, Suzuki T, Tsuchiya M, Satoh S, Ikegaki I, Shibuya M, Suzuki Y, Hidaka H. (1989) "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase." Br J Pharmacol. 98(4):1091-100.

Seto M, Sasaki Y, Hidaka H, Sasaki Y. (1991) "Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle." Eur J Pharmacol. 195(2):267-72.

Takizawa S, Hori M, Ozaki H, Karaki H. (1993) "Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle." Eur J Pharmacol. 250(3):431-7.

Seto M, Shindo K, Ito K, Sasaki Y (1995) "Selective inhibition of myosin phosphorylation and tension of hyperplastic arteries by the kinase inhibitor HA1077" Eur. J. Pharmacol. 276(1-2):27-33

Satoh S, Ikegaki I, Suzuki Y, Asano T, Shibuya M, Hidaka H (1996) "Neuroprotective properties of a protein kinase inhibitor against ischaemia-induced neuronal damage in rats and gerbils" Br. J. Pharmacol. 118(7):1592-6

Negoro N, Hoshiga M, Seto M, Kohbayashi E, Ii M, Fukui R, Shibata N, Nakakoji T, Nishiguchi F, Sasaki Y, Ishihara T, Ohsawa N (1999) "The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells" Biochem. Biophys. Res. Commun. 262(1):211-5

Sward K, Dreja K, Susnjar M, Hellstrand P, Hartshorne DJ, Walsh MP (2000) "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum" J. Physiol. 522 Pt 1:33-49

Chrissobolis S, Sobey CG (2001) "Evidence that Rho-kinase activity contributes to cerebral vascular tone in vivo and is enhanced during chronic hypertension: comparison with protein kinase C" Circ. Res. 88(8):774-9

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.