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Y-27632, free base (CAS 146986-50-7)

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Alternate Names:
Y-27632, free base is also known as ROCK Inhibitor.
Application:
Y-27632, free base is the free base form of Y-27632 dihydrochloride and a novel and specific inhibitor of Rho-associated kinases.
CAS Number:
146986-50-7
Purity:
98%
Molecular Weight:
247.34
Molecular Formula:
C14H21N3O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Y-27632, free base, also known as ROCK Inhibitor, is a novel and specific inhibitor of Rho-associated kinases (p160ROCK). Y-27632, free base is cell permeable and inhibits ROCK-I and ROCK-II (IC50=800 nM) by competing with ATP and on cultured human cells mimics the effects of β-agonists. In Swiss 3T3 cells Y-27632, free base abolished stress fibers but did not affect G1-S phase transition at 10 µM. Y-27632, free base has been used to increase survival of human embryonic stem cells as well as display cardioprotective effects. Y-27632, free base has been observed to act on smooth muscle contractions and myosin phosphorylation by inhibiting agonist induced Ca2+ sensitization as well as K+-induced contractions, in vascular smooth muscle. In rat ascites hepatoma (MM1) cells Y-27632, free base had suppressed, through regulation of focal adhesion and focal adhesion kinase, tumor cell invasion.


Y-27632, free base (CAS 146986-50-7) References

  1. Signaling from Rho to the actin cytoskeleton through protein kinases ROCK and LIM-kinase.  |  Maekawa, M., et al. 1999. Science. 285: 895-8. PMID: 10436159
  2. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases.  |  Ishizaki, T., et al. 2000. Mol Pharmacol. 57: 976-83. PMID: 10779382
  3. A p160ROCK-specific inhibitor, Y-27632, attenuates rat hepatic stellate cell growth.  |  Iwamoto, H., et al. 2000. J Hepatol. 32: 762-70. PMID: 10845663
  4. Y-27632, an inhibitor of rho-associated protein kinase, suppresses tumor cell invasion via regulation of focal adhesion and focal adhesion kinase.  |  Imamura, F., et al. 2000. Jpn J Cancer Res. 91: 811-6. PMID: 10965022
  5. The effect of a Rho kinase inhibitor Y-27632 on superoxide production, aggregation and adhesion in human polymorphonuclear leukocytes.  |  Kawaguchi, A., et al. 2000. Eur J Pharmacol. 403: 203-8. PMID: 10973620
  6. Specificity and mechanism of action of some commonly used protein kinase inhibitors.  |  Davies, SP., et al. 2000. Biochem J. 351: 95-105. PMID: 10998351
  7. Use and properties of ROCK-specific inhibitor Y-27632.  |  Narumiya, S., et al. 2000. Methods Enzymol. 325: 273-84. PMID: 11036610
  8. Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxide-independent pathway.  |  Chitaley, K., et al. 2001. Nat Med. 7: 119-22. PMID: 11135626
  9. Inhibition of intrahepatic metastasis of human hepatocellular carcinoma by Rho-associated protein kinase inhibitor Y-27632.  |  Takamura, M., et al. 2001. Hepatology. 33: 577-81. PMID: 11230737
  10. Inhibition of high K+-induced contraction by the ROCKs inhibitor Y-27632 in vascular smooth muscle: possible involvement of ROCKs in a signal transduction pathway.  |  Sakamoto, K., et al. 2003. J Pharmacol Sci. 92: 56-69. PMID: 12832856
  11. Comparison of effects of Y-27632 and Isoproterenol on release of cytokines from human peripheral T cells.  |  Aihara, M., et al. 2003. Int Immunopharmacol. 3: 1619-25. PMID: 14555287
  12. Y-27632, a Rho-kinase inhibitor, inhibits proliferation and adrenergic contraction of prostatic smooth muscle cells.  |  Rees, RW., et al. 2003. J Urol. 170: 2517-22. PMID: 14634463
  13. Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity.  |  Breitenlechner, C., et al. 2003. Structure. 11: 1595-607. PMID: 14656443
  14. Preventive effect of Y-27632, a selective Rho-kinase inhibitor, on ischemia/reperfusion-induced acute renal failure in rats.  |  Teraishi, K., et al. 2004. Eur J Pharmacol. 505: 205-11. PMID: 15556154
  15. Rho-kinase inhibitor, Y-27632, has an antinociceptive effect in mice.  |  Büyükafşar, K., et al. 2006. Eur J Pharmacol. 541: 49-52. PMID: 16750189
  16. Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y-27632.  |  Yamaguchi, H., et al. 2006. J Biochem. 140: 305-11. PMID: 16891330
  17. Molecular characterization of the effects of Y-27632.  |  Darenfed, H., et al. 2007. Cell Motil Cytoskeleton. 64: 97-109. PMID: 17009325
  18. A Rho-kinase inhibitor, Y-27632, reduces cholinergic contraction but not neurotransmitter release.  |  Fernandes, L., et al. 2006. Eur J Pharmacol. 550: 155-61. PMID: 17010334
  19. FAP-α (Fibroblast activation protein-α) is involved in the control of human breast cancer cell line growth and motility via the FAK pathway.  |  Jia, J., et al. 2014. BMC Cell Biol. 15: 16. PMID: 24885257
  20. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension.  |  Uehata, M., et al. 1997. Nature. 389: 990-4. PMID: 9353125
  21. Molecular dissection of the Rho-associated protein kinase (p160ROCK)-regulated neurite remodeling in neuroblastoma N1E-115 cells.  |  Hirose, M., et al. 1998. J Cell Biol. 141: 1625-36. PMID: 9647654

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Y-27632, free base, 5 mg

sc-3536
5 mg
$182.00

Y-27632, free base, 50 mg

sc-3536A
50 mg
$693.00

What is the solubility of this product?

Asked by: SCchem16
Thank you for your question. Y-27632, free base, sc-3536, is soluble in water at >25 mg/ml.
Answered by: TechService7
Date published: 2017-02-14
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Rated 5 out of 5 by from JiaJia, et. al. (PubMed ID 24885257) used product sc-3536 in the course of studying the influence of inhibitors on the signaling pathway on adhesion and migration of breast cancer cells. -SCBT Publication Review
Date published: 2015-06-10
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Y-27632, free base is rated 5.0 out of 5 by 1.
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