Replaces Prod. #: ALX-270-071
Inhibits Rho kinase (ROCK; Ki=0.33μM). Selective protein kinase A and G inhibitor (both Ki’s = 1.6μM). Inhibits agonist-induced activation of NADPH oxidase in human neutrophils (IC50=15μM). Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ. Cell permeable Ca2+ antagonist with antivasospastic properties.
Product Details
| Alternative Name: | 1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl, Fasudil |
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| Formula: | C14H17N3O2S . 2HCl |
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| MW: | 364.3 |
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| CAS: | 103745-39-7 |
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| MI: | 14: 3942 |
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| Purity: | ≥98% (TLC) |
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| Identity: | Determined by 1H-NMR and MS. |
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| Appearance: | White to off-white solid. |
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| MeltingPoint: | 238-242°C |
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| Solubility: | Soluble in water (>20mg/ml), methanol or DMSO. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 1 year after receipt when stored, as supplied, at 0-4°C. Stock solutions are stable for up to 3 months at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
PAX9 regulates periodontal ligament stem cell-like differentiation of human induced pluripotent stem cells: R. Sugiura, et al.; Biomedicines
10, 2366 (2022),
Abstract;
Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells: Y. Kaneko, et al.; Sci. Rep.
6, 19640 (2016),
Application(s): Cell culture,
Abstract;
Full Text
Effects of HA-1077 and Y-27632, Two Rho-Kinase Inhibitors, in the Human Umbilical Artery: M. Ark, et al.; Cell Biochem. Biophys.
41, 331 (2004),
Abstract;
Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCbetaI, PKCbetaII and PKCzeta in human neutrophils: X. Siomboing, et al.; Mediators Inflamm.
10, 315 (2001),
Abstract;
Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells: H. Nagumo, et al.; Am. J. Physiol. Cell. Physiol.
278, C57 (2000),
Abstract;
Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension: U. M. Ishizaki, et al.; Nature
389, 990 (1997),
Abstract;
Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle: S. Takizawa, et al.; Eur. J. Pharmacol.
250, 431 (1993),
Abstract;
Inhibition by the protein kinase inhibitor HA1077 of the activation of NADPH oxidase in human neutrophils.: M. Arai, et al.; Biochem. Pharmacol.
46, 1487 (1993),
Abstract;
A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture: M. Shirotani, et al.; J. Pharmacol. Exp. Ther.
259, 738 (1991),
Abstract;
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle: M. Seto, et al.; Eur. J. Pharmacol.
195, 267 (1991),
Abstract;
Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator: Y. Sasaki & Y. Sasaki; BBRC
171, 1182 (1990),
Abstract;
Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase: T. Asano, et al.; Br. J. Pharmacol.
98, 1091 (1989),
Abstract;
The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs: O. Shibuya, et al.; Acta Neurochir.
90, 53 (1988),
Abstract;
Mechanism of action of a novel antivasospasm drug, HA1077: T. Asano, et al.; J. Pharmacol. Exp. Ther.
241, 1033 (1987),
Abstract;
