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Y-27632, free base | CAS 146986-50-7 | SCBT - Santa Cruz Biotechnology
Y-27632, free base CAS: 146986-50-7
MF: C14H21N3O
MW: 247.34

Y-27632, free base (CAS 146986-50-7)

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备用名: Y-27632, free base is also known as ROCK Inhibitor.
应用; Y-27632, free base is the free base form of Y-27632 dihydrochloride and a novel and specific inhibitor of Rho-associated kinases.
CAS号码: 146986-50-7
纯度: 98%
分子量: 247.34
分子式: C14H21N3O
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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Y-27632, free base 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.


参考文献

  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

物理状态 :
Solid
保存 :
Store at -20° C
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
SMILES :
C[[email protected]](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N

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