HA-1077

BML-EI233

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Rho kinase (ROCK) inhibitor

Inhibits Rho kinase (ROCK; K_i=0.33μM). Selective protein kinase A and G inhibitor (both K_i’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.

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Product Details

Alternative Name	1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl, Fasudil
Appearance	White to off-white solid.
CAS	103745-39-7
Couple Target	CaM kinase, MLCK, PKA, PKG, ROCK
Couple Type	Inhibitor
Formula	C₁₄H₁₇N₃O₂S . 2HCl
Identity	Determined by 1H-NMR and MS.
MI	14: 3942
MW	364.3
MeltingPoint	238-242°C
Purity	≥98% (TLC)
Solubility	Soluble in water (>20mg/ml), methanol or DMSO.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. 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.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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

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HA-1077

BML-EI233

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