ROCK INHIBITOR
Y-27632 dihydrochloride
CAS: 129830-38-2
Molecular Formula: C14H23Cl2N3O
ROCK INHIBITOR - Names and Identifiers
ROCK INHIBITOR - Physico-chemical Properties
| Molecular Formula | C14H23Cl2N3O |
| Molar Mass | 320.25792 |
| Melting Point | 258℃ |
| Solubility | DMSO:64 mg/mL warmed (199.83 mM);Water:14 mg/mL (43.71 mM);Ethanol Insoluble |
| Appearance | Morphological powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or methanol may be stored at -20° for up to 3 months. |
| MDL | MFCD03490488 |
| Physical and Chemical Properties | Bioactive Y-27632 2HCl is a selective ROCK1(p160ROCK) inhibitor. Ki is 140 nM in cell-free test, which is more than 200 times stronger than other kinases including PKC,cAMP-dependent protein kinase, MLCK and PAK. |
| Use | Product Description Y-27632 2HCl is a selective ROCK1(p160ROCK) inhibitor, Ki is 140 nM, which is more than 200 times more selective than acting on other kinases, including PKC,cAMP-dependent protein kinase, MLCK and PAK. The target ROCK1 ROCK2IC50140 nM (Ki) 300 nM (Ki)In VitroY-27632 is equally effective in inhibiting ROCK-II. Y-27632 acting on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK) had little activity with Ki of 26 μM, 25 μM, and> amp; gt; 250 μM, respectively. Y-27632 inhibit various stimulants instead of KCl, including Phenylephrine, Histamine, Acetylcholine, Serotonin, Endothelin, and Thromboxane-induced smooth muscle contraction by selectively inhibiting Ca2 + sensitization, IC50 is 0.3-1 μM. Y-27632 acts on cultured cells to inhibit Rho-induced, p160ROCK-regulated stress fiber formation. Y-27632 treatment blocks the activation of Rho-regulated actomyosin and also blocks the invasion activity of MM1 cells stimulated by LPA, which is concentration-dependent. Human embryonic stem cells (hES) treated with 10 μM Y-27632 in serum-free suspension (SFEB) medium significantly reduced separation-induced apoptosis, improved cloning efficiency (from ~ 1% to ~ 27%), promoted subcloning after transgene, and allowed SFEB cultured hES cells to survive and differentiate into Bf1 + cortical and basal progenitor cells. In VivoY-27632 treated spontaneously hypertensive rats, renal hypertensive rats and deoxycorticosterone acetic acid (DOCA) salt hypertensive rats orally at a dose of 30 mg/kg significantly reduced blood pressure, which was dose-dependent. Y-27632 rats expressing Val14-RhoA were continuously treated by implantation pump at 0.55 μL per hour for 11 days, delaying MM1 cell invasion. Y-27632 acts on the pulmonary circulation to reduce hypoxia-induced angiogenesis and vascular remodeling by inhibiting ROCK. |
| In vitro study | Y-27632 is equally effective in inhibiting ROCK-II. Y-27632 had little activity on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK), with K I of 26 μm, 25 μm, and> 250 μm, respectively. Y-27632 blocking Rho-regulated actomyosin activation by selective inhibition of Ca Y-27632 treatment also blocks LPA-stimulated MM1 cell invasion activity in a concentration-dependent manner. 10 μm Y-27632 treatment of human embryonic stem cells (hES) in serum-free suspension (SFEB) media significantly reduced isolation-induced apoptosis, cloning efficiency was increased (from -1% to-27%), subcloning was promoted after transgene, and SFEB-cultured hES cells survived and differentiated into Bf1 + cortical and basal telencephalon progenitor cells. |
| In vivo study | Y-27632 according to the dose of 30 mg/kg oral treatment of spontaneously hypertensive rats, renal hypertensive rats, and deoxycorticosterone acetate (DOCA) salt hypertensive rats, significantly reduced blood pressure, this effect is dose dependent. Y-27632 expression Val was treated continuously at 0.55 μl/hr by implanted pump Y-27632 acts on the pulmonary circulation, reduces hypoxia-induced angiogenesis, and vascular remodeling by inhibiting ROCK. |
ROCK INHIBITOR - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | 36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
| HS Code | 29333990 |
ROCK INHIBITOR - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.122 ml | 15.612 ml | 31.225 ml |
| 5 mM | 0.624 ml | 3.122 ml | 6.245 ml |
| 10 mM | 0.312 ml | 1.561 ml | 3.122 ml |
| 5 mM | 0.062 ml | 0.312 ml | 0.624 ml |
Last Update：2024-01-02 23:10:35
ROCK INHIBITOR - Reference Information
| biological activity | Y-27632 2HCl is a selective ROCK1(p160ROCK) inhibitor. Ki is 140 nM in cell-free test, which is more than 200 times stronger than other kinases including PKC,cAMP-dependent protein kinase, MLCK and PAK. |
| target | TargetValue ROCK1 (p160ROCK) (cell-free assessment) 140 nM (ki) ROCK2 (cell-free assessment) 300 nM (ki) |
| Target | Value |
| ROCK1 (p160ROCK) (Cell-free assay) | 140 nM(Ki) |
| ROCK2 (Cell-free assay) | 300 nM(Ki) |
| in vitro studies | Y-27632 are equally effective in inhibiting ROCK-II. Y-27632 acting on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK) had little activity, with K I being 26 μM, 25 μM, and> amp; gt; 250 μM, respectively. Y-27632 block the activation of Rho-regulated actomyosin and LPA-stimulated MM1 cell invasion activity by selectively inhibiting Ca Y-27632 treatment, which is concentration-dependent. Human embryonic stem cells (hES) treated with 10 μM Y-27632 in serum-free suspension (SFEB) medium significantly reduced separation-induced apoptosis, improved cloning efficiency (from ~ 1% to ~ 27%), promoted subcloning after transgene, and allowed SFEB cultured hES cells to survive and differentiate into Bf1 + cortical and basal progenitor cells. |
| in vivo study | Y-27632 orally treated spontaneously hypertensive rats, renal hypertensive rats and deoxycorticosterone acetic acid (DOCA) salt hypertensive rats at a dose of 30 mg/kg, significantly reducing blood pressure, which is dose-dependent. Y-27632 0.55 μL per hour, Val Y-27632 is continuously treated by implantation pump to act on pulmonary circulation, and hypoxia-induced angiogenesis and vascular remodeling are reduced by inhibiting ROCK. |
Last Update：2024-04-10 22:29:15
ROCK INHIBITOR - Uses and synthesis methods
Target
Target Value
ROCK1 (p160ROCK)
(Cell-free assay) 140 nM(Ki)
ROCK2
(Cell-free assay) 300 nM(Ki)
in vitro studies
Y-27632 is equally effective in inhibiting ROCK-II. Y-27632 acting on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK) had little activity, with K I being 26 μM, 25 μM, and> amp; gt; 250 μM, respectively. Y-27632 block the activation of Rho-regulated actomyosin and LPA-stimulated MM1 cell invasion activity by selectively inhibiting Ca Y-27632 treatment, which is concentration-dependent. Human embryonic stem cells (hES) treated with 10 μM Y-27632 in serum-free suspension (SFEB) medium significantly reduced separation-induced apoptosis, improved cloning efficiency (from ~ 1% to ~ 27%), promoted subcloning after transgene, and allowed SFEB cultured hES cells to survive and differentiate into Bf1 + cortical and basal progenitor cells.
In vivo studies
Y-27632 orally treated spontaneously hypertensive rats, renal hypertensive rats, and deoxycorticosterone acetic acid (DOCA) salt hypertensive rats at a dose of 30 mg/kg significantly reduced blood pressure, which was dose-dependent. Y-27632 0.55 μL per hour, Val Y-27632 is continuously treated by implantation pump to act on pulmonary circulation, and hypoxia-induced angiogenesis and vascular remodeling are reduced by inhibiting ROCK.
Last Update：2024-04-10 22:29:15
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Product Name: Y-27632 dihydrochloride Visit Supplier Webpage Request for quotationCAS: 129830-38-2
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Spot supply
Product Name: Y-27632 dihydrochloride Visit Supplier Webpage Request for quotationCAS: 129830-38-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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