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Home > Products >  Y-27632 2HCl

Y-27632 2HCl CAS NO.129830-38-2

  • Min.Order: 2 Metric Ton
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  • Product Details

Keywords

  • Y-27632 2HCl
  • ROCK inhibitor
  • 129830-38-2

Quick Details

  • ProName: Y-27632 2HCl
  • CasNo: 129830-38-2
  • Molecular Formula: C14H21N3O.2HCl
  • ProductionCapacity: Metric Ton/Day
  • Purity: >97%
  • LimitNum: 2 Metric Ton

Superiority

Biological Activity

 

Description Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Targets
ROCK1 (p160ROCK) [1]
(Cell-free assay)
ROCK2 [6]
(Cell-free assay)
140 nM(Ki) 300 nM(Ki)
In vitro

Y-27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively, as well as PKA activated by another Rho-family GTPase member, Cdc42. Y-27632 2HCl inhibits smooth-muscle contraction induces by various agonists including phenylephrine, histamine, acetylcholine, serotonin, endothelin, and thromboxane with IC50 of 0.3-1 μM, by selectively inhibiting Ca2+ sensitization. Y-27632 2HCl suppresses Rho-induced, p160ROCK-mediated formation of stress fibres in cultured cells. [1] Y-27632 2HCl treatment blocks both Rho-mediated activation of actomyosin and LPA-stimulated invasive activity of MM1 cells in a concentration-dependent manner. [2] Y-27632 2HCl treatment is not only sufficient to initiate formation of exuberant axonal processes but also facilitates axonal maturation during the very early stages of axonogenesis, while largely sparing axon elongation. [3] In human embryonic stem (hES) cells, Y-27632 2HCl treatment at 10 μM markedly diminishes dissociation-induced apoptosis even in serum-free suspension (SFEB) culture, increases cloning efficiency (from ~1% to ~27%), facilitates subcloning after gene transfer, and enables SFEB-cultured hES cells to survive and differentiate into Bf1+ cortical and basal telencephalic progenitors. [4]

Cell Data
 
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Salivary gland stem cells Function Assay 10 µM 7 d   Reduces SGSC senescence 25804560
HT22 Cytotoxic Assay 10 µM 13 h   Protects against glutamate-induced neuronal death 22810835
Swiss3T3 Colony-forming Assay 10 µM 13 d   Increases prostate cell colony-forming activity 21464902

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western Blot               24704720 26555939 27399334
Transwell migration assay 27694793
Immunofluorescence       21362567 24523903 27399334
Growth inhibition assay 24523903
ELISA 30320378
In vivo Oral administration of Y-27632 2HCl at 30 mg/kg significantly decreases the blood pressure in a dose-dependent manner in spontaneous hypertensive rats, renal hypertensive rats, as well as deoxycorticosterone acetate (DOCA)-salt hypertensive rats. [1] When Y-27632 2HCl is continuously administered at a rate of 0.55 μL per hour by implanted pumps for 11 days tumor cell invasion (MM1 cells expressing Val14-RhoA in rats) is significantly delayed. [2] By inhibiting ROCK, Y-27632 2HCl treatment attenuates hypoxia-induced angiogenesis and vascular remodeling in the pulmonary circulation. [5] Pretreatment with Y-27632 has a protective effect against tumor formation in albino mice with Ehrlich ascites carcinoma. [7]

 

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