Y-5301 Y-27632, Dihydrochloride Salt, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 160 mg/mL; soluble in ethanol at 12 mg/mL with warming; soluble in water at 90 mg/mL; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

YXX-105 YXX-104 YXX-103 YXX-102 YXX-101

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• More than 150 labs worldwide have purchased Y-27632 from LC Labs (either directly from us or from our many distributors, many of whom resell under their own labels).
• Y-27632 is a novel and specific Rho-associated coiled-coil forming protein kinase (ROCK) inhibitor. Narumiya, S., et al. "Use and properties of ROCK-specific inhibitor Y-27632." Methods Enzymol. 325: 273-284 (2000).
• This research compound is the dihydrochloride salt form of Y-27632. We also plan to offer the free base form; please see Y-27632, Free Base, Cat. No. Y-5399.
• Y-27632 inhibited ROCK-I (Ki = 0.22 µM) and ROCK-II (Ki = 0.30 µM) by competing with ATP for its binding to the kinase. Ishizaki, T., et al. "Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases." Mol. Pharmacol. 57: 976-983 (2000).
• Y-27632 selectively inhibited Ca2+ sensitization of smooth muscle and blocked its contraction, prevented Rho-induced, p160ROCK-mediated formation of stress fibers in cultured cells, and dramatically lowered hypertension in several hypertensive rat models. Uehata, M., et al. "Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension." Nature 389: 990-994 (1997).
• Y-27632 inhibited cell transformation mediated by RhoA and its guanine-nucleotide exchange factor (GEF). Sahai, E., et al. "Transformation mediated by RhoA requires activity of ROCK kinases." Curr. Biol. 9: 136-145 (1999).
• Y-27632 inhibited both Rho-mediated activation of actomyosin and invasive activity of rat MM1 hepatoma cells. Continuous delivery of Y-27632 largely prevented the dissemination of MM1 cells implanted into the peritoneal cavity of syngeneic rats. Itoh, K., et al. "An essential part for Rho-associated kinase in the transcellular invasion of tumor cells." Nat. Med. 5: 221-225 (1999).
• Y-27632 blocked chemotactic peptide-induced development of cell polarity and locomotion, and inhibited myosin light chain phosphorylation with similar potency (ED50 = 0.5-1.1 µM). Niggli, V. "Rho-kinase in human neutrophils: a role in signalling for myosin light chain phosphorylation and cell migration." FEBS Lett. 445: 69-72 (1999).
• Y-27632 had antinociceptive properties, possibly by inhibition of Rho-kinase. Buyukafsar, K., et al. "Rho-kinase inhibitor, Y-27632, has an antinociceptive effect in mice." Eur. J. Pharmacol. 541: 49-52 (2006).
• Y-27632 blocked the development of ischemia/reperfusion-induced acute renal failure, possibly by inhibiting myeloperoxidase activity in an early phase after reperfusion. Teraishi, K., et al. "Preventive effect of Y-27632, a selective Rho-kinase inhibitor, on ischemia/reperfusion-induced acute renal failure in rats." Eur. J. Pharmacol. 505: 205-211 (2004).
• Y-27632 prevented intrahepatic metastasis of human hepatocellular carcinoma. Takamura, M., et al. "Inhibition of intrahepatic metastasis of human hepatocellular carcinoma by Rho-associated protein kinase inhibitor Y-27632." Hepatology 33: 577-581 (2001).
• Y-27632 inhibited both of lysophosphatidic acid (LPA)- and fibronectin (FN)-induced migration and morphological change of rat ascites hepatoma (MM1) cells. It impaired LPA- and FN-evoked formation of focal adhesions and actin bundles and suppressed LPA- and FN-induced tyrosine phosphorylation of focal adhesion kinase and paxillin in MM1 cells. Imamura, F., et al. "Y-27632, an inhibitor of rho-associated protein kinase, suppresses tumor cell invasion via regulation of focal adhesion and focal adhesion kinase." Jpn. J. Cancer Res. 91: 811-816 (2000).
• This Y-27632 product is the dihydrochloride salt, whose CAS number is given above. The CAS number of the free base form is 146986-50-7.
• Related CAS number: 331752-47-7 for Y-27632 diHCl salt monohydrate.
• A CAS number previously assigned to Y-27632 diHCl salt monohydrate, namely 203911-23-3, has been deleted by CAS and is no longer in use, and a CAS number previously assigned to Y-27632, Free Base, namely 742043-06-7, has also been deleted by CAS and is also no longer in use.
• As of October 2013, many other vendors (Adipogen, Affix, AG Scientific, BioVision, Calbiochem/EMD, Cellagen, Enzo, MyBioSource, Reagents Direct, Santa Cruz, VDM Biochemicals, etc.) are incorrectly using CAS number 146986-50-7 for the diHCl or diHCl monohydrate salt forms of Y-27632. Chemical Abstracts Service has assigned the CAS number 146986-50-7 to the free base form only.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.