Product nameHA-1077 (Fasudil), ROCK2 inhibitor
Biological descriptionROCK2 inhibitor (IC50 = 1.9 µM). Also shown to inhibit PRK2 (IC50 = 4 µM), MSK1 (IC50 = 5 µM), Rsk2 (IC50 = 15 µM), PKA, p70 S6 Kinase, CaM Kinase and MLCK. Calcium antagonist and vasodilator.
Also available in simple stock solutions (ab146700) - add 1 ml of water to get an exact, ready-to-use concentration.
Chemical name1-(5-Isoquinolinylsulfonyl)homopiperazine hydrochloride
Storage instructionsStore at Room Temperature. The product can be stored for up to 12 months.
Solubility overviewSoluble in water to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Toxic, refer to SDS for further information.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Our Abpromise guarantee covers the use of ab120306 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
|Functional Studies||Use at an assay dependent concentration.|
ab46154 staining VEGF in MCF7 cells treated with HA 1077 (ab120306), by ICC/IF. Decrease in VEGF expression correlates with increased concentration of HA 1077 as described in literature.
The cells were incubated at 37°C for 1h in media containing different concentrations of ab120306 (HA 1077) in DMSO, fixed with 100% methanol for 5 minutes at -20°C and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab46154 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody.
This product has been referenced in:
- Bain J et al. The selectivity of protein kinase inhibitors: a further update. Biochem J 408:297-315 (2007). Read more (PubMed: 17850214) »
- Davies SP et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351:95-105 (2000). Read more (PubMed: 10998351) »
- Amano M et al. The COOH terminus of Rho-kinase negatively regulates rho-kinase activity. J Biol Chem 274:32418-24 (1999). Read more (PubMed: 10542285) »
- Asano T & Hidaka H New pharmacological strategies in vascular diseases: a novel intracellular calcium antagonist, HA1077 (AT-877) and cerebral vasospasm. Methods Find Exp Clin Pharmacol 12:443-8 (0). Read more (PubMed: 2087143) »