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Home / Biochemicals / Small Molecules

HA-1077

SKU : BHB21300171

A Rho/Rok Inhibitor

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Alomone Labs

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Mfr.No.	H-220, H-220_10 mg, H-220_5 mg
Description	HA-1077 (#H-220) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C14H17N3O2S2HCl.
Synonyms	Synthetic
Background	HA-1077 is a small, cell permeable derivative of isoquinoline which specifically inhibits the small GTPase - Rho by inhibition of its associated kinase-Rho dependent kinase (ROK). This signaling pathway acts as a molecular switch to control cytoskeleton organization in many cell types including smooth muscle.1-3 By inhibition of ROK, HA-1077 decreases the myosin light chain (MLC) phosphorylation induced by Ca2+ due to abrogating Rho-mediated inhibition of MLC dephosphorylation. HA-1077 also inhibits fetal calf serum-induced proliferation and (3H)thymidine incorporation into DNA of growth-arrested VSMC in a dose-dependent manner.4-6At concentrations higher than 5 uM, it induces disorganization of actin filament structure. This compound was also found to act as a vasodilator and antivasospasm drug which antagonizes the verapamil-insensitive voltage dependent Ca2+ channel and is used clinically for treatment of the cerebral vasospasm after subarachnoid hemorrhage.7-9
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	>1 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. For long-term storage of diluted solutions, we recommend adding 0.1% BSA. Repeat freeze-thawing may result in loss of activity.
Cas Number	103745-39-7
Molecular Weight	364.3
Solubility	Water, DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	Rho/Rok
Activity	HA-1077 specifically inhibits the small GTPase - Rho through its associated kinase-Rho dependent kinase (ROK), thereby inhibiting myosin llight chain (MLC) phosphorylation1-3. It also acts as an intracellular Ca2+ antagonist4.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: 1-(5-Isoquinolinesulfonyl) homopiperazine, dihydrochloride salt.

Purity	>99%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: Up to two weeks at 4°C or six months at -20°C.

Product Manual	SDS

Reference	Asano, T. et al. (1989) Br. J. Pharmacol. 98, 1091. Uehata, M. et al. (1997) Nature 389, 990. Nagumo, H. et al.(2000) Am. J. Physiol. Cell Physiol. 278, C57. Shirotani, M. et al. (1991) J. Pharmacol. Exp. Ther. 259, 738. Sasaki, Y. et al. (1987) Am. J. Physiol. 253, C71. Seto, M. et al. (1991) Eur. J. Pharmacol. 195, 267. Asano, T. et al. (1987) J. Pharmacol. Exp. Ther. 241, 1033. Takayasu, M. et al. (1986) J. Neurosurg. 65, 80. Takizawa, S. et al. (1993) Eur. J. Pharmacol. 250, 431. Asano, T. et al. (1989) Br. J. Pharmacol. 98, 1091. Uehata, M. et al. (1997) Nature 389, 990. Nagumo, H. et al.(2000) Am. J. Physiol. 278, C57. Takayasu, M. et al. (1989) J. Neurosurg. 65, 80.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300171-1	H-220_10 mg	10 mg	$354		Add to Cart
BHB21300171-2	H-220_5 mg	5 mg	$223		Add to Cart
BHB21300171-3	H-220_5 mg	5x5 mg	$879		Add to Cart

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