Dichlorhydrate Y-27632 est un inhibiteur de ROCK-I et de ROCK-II qui est actif par voie orale et ATP-compétitif, avec Kis de 220 et 300 nM, respectivement. Dichlorhydrate Y-27632 induit l'apoptose. Dichlorhydrate Y-27632 amorce les cellules souches pluripotentes induites par l'homme (hIPSC) pour se différencier sélectivement vers la lignée mésendodermique via une modulation de type transition épithéliale-mésenchymateuse.
Y-27632 Dihydrochlorid ist ein oral wirksamer, ATP-kompetitiver Inhibitor von ROCK-I und ROCK-II mit einem Kis-Wert von 220 bzw. 300 nM. Y-27632 Dihydrochlorid induziert apoptosis. Y-27632 Dihydrochlorid veranlasst humane induzierte pluripotente Stammzellen (hIPSCs), sich selektiv über epithelial-mesenchymale Übergangs-ähnliche Modulation in Richtung mesendodermale Abstammung zu differenzieren.
Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.
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Y-27632 dihydrochloride Chemical Structure
CAS No. : 129830-38-2
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Based on 270 publication(s) in Google Scholar
Other Forms of Y-27632 dihydrochloride:
Y-27632
In-stock
Y-27632 dihydrochloride (GMP)
In-stock
Y-27632 dihydrochloride (Standard)
In-stock
Y-27632 hydrochloride hydrate
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Y-27632 dihydrochloride purchased from MedChemExpress. Usage Cited in:
Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.
[Abstract]
Expression of CTC cluster-related (plakoglobin and CD44) and EMT-related (vimentin and E-cadherin, 4 days) proteins in LNCaP cells grown on different substrates after treatment with different inhibitors (Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl)).
Y-27632 dihydrochloride purchased from MedChemExpress. Usage Cited in:
Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.
[Abstract]
Immunofluorescence imaging of LNCaP cells treated with the Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl). After the cells are cultured on different substrates for 3 days, inhibitors are added and incubated for 24 h.
Y-27632 dihydrochloride purchased from MedChemExpress. Usage Cited in:
J Exp Clin Cancer Res. 2018 Jun 28;37(1):128.
[Abstract]
MHCC-97H and Huh-7 cells co-transfected with control or supervillin-specific siRNA and a RhoA(WT), RhoA(V14), or RhoA(N19) plasmids for 48 h are treated with PBS or Y27632 2HCl (10 μM) for 16 h during hypoxia, and then assayed for phosphorylated p38 and ERK by immunoblotting. β-actin is used as the loading control
SKOV3 mock-transfected control (Ctrl) and shRNA-Hic-5 knockdown (KD) (sh-S1 and sh-S2) cells were either untreated (-) or treated (+) with 10mM Y27632 over a period of 48 hr. SKOV3 mock-transfected control (Ctrl) and shRNA-Hic-5 knockdown (KD) (sh-S1 and sh-S2) clones were either untreated (-) or treated (+) with 10 mM Y27632 followed by stimulation without (-) or with (+) 5 ng/mL of TGFβ1 for 48 hr.
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Description
Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects[1][2][3][4].
IC50 & Target[1]
ROCK-I
220 nM (Ki)
ROCK-II
300 nM (Ki)
PKN
3.1 μM (Ki)
Citron kinase
5.3 μM (Ki)
PKCα
73 μM (Ki)
PKA
25 μM (Ki)
In Vitro
Y-27632 (1-5 μM; 0-60 min) promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs) [3].
Y-27632 (1-5 μM; 0-60 min) induces the expression of NSE, MAP-2 and nestin in ADSCs [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Y-27632 dihydrochloride Related Antibodies
Western Blot Analysis[3]
Cell Line:
Adipose tissue-derived stem cells (ADSCs)
Concentration:
20 μM
Incubation Time:
24 hours
Result:
Resulted in the up-regulation of NSE, MAP-2 and nestin protein levels by 25.3, 3.1 and 2.5 fold, respectively, compared to control cells not treated by Y-27632.
In Vivo
Y-27632 (oral gavage; 30 mg/kg; once daily; 4 w) prevents dimethylnitrosamine-induced hepatic fibrosis in rats[1].
Y-27632 (oral gavage; 5-10 mg/kg; once) shows antiepileptic effects in epilepsy induced by PTZ and MES[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Wistar rats injected with dimethylnitrosamine[1]
Dosage:
30 mg/kg
Administration:
Oral gavage; 30 mg/kg; once daily; 4 weeks
Result:
Decreased the occurrence of dimethylnitrosamine-induced hepatic fibrosis and reduced the collagen and hydroxyproline content and α-smooth muscle actin expression in the liver.
Animal Model:
Male Swiss albino mice injected with PTZ (pentylenetetrazole) or induced by MES (maximal electroconvulsive shock)[2]
Dosage:
5-10 mg/kg
Administration:
Oral gavage; 5-10 mg/kg; once
Result:
Prolonged the onset time of myoclonic jerks when compared with those observed in the saline group (P<0.05).
Prolonged the onset time of clonic convulsions when compared with saline group (P<0.05).
Prevented the occurrence of tonic hindlimb extensions and death.
DMSO : 50 mg/mL (156.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.1225 mL
15.6123 mL
31.2246 mL
5 mM
0.6245 mL
3.1225 mL
6.2449 mL
10 mM
0.3122 mL
1.5612 mL
3.1225 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: PBS
Solubility: 220 mg/mL (686.94 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
[1]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.
[Content Brief]
[2]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.
[Content Brief]
[3]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells. Chin Med J (Engl). 2012 Sep;125(18):3332-5.
[Content Brief]
[4]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
[Content Brief]
[1]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.
[2]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.
[3]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells. Chin Med J (Engl). 2012 Sep;125(18):3332-5.
[4]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO / H2O
1 mM
3.1225 mL
15.6123 mL
31.2246 mL
78.0616 mL
5 mM
0.6245 mL
3.1225 mL
6.2449 mL
15.6123 mL
10 mM
0.3122 mL
1.5612 mL
3.1225 mL
7.8062 mL
15 mM
0.2082 mL
1.0408 mL
2.0816 mL
5.2041 mL
20 mM
0.1561 mL
0.7806 mL
1.5612 mL
3.9031 mL
25 mM
0.1249 mL
0.6245 mL
1.2490 mL
3.1225 mL
30 mM
0.1041 mL
0.5204 mL
1.0408 mL
2.6021 mL
40 mM
0.0781 mL
0.3903 mL
0.7806 mL
1.9515 mL
50 mM
0.0624 mL
0.3122 mL
0.6245 mL
1.5612 mL
60 mM
0.0520 mL
0.2602 mL
0.5204 mL
1.3010 mL
80 mM
0.0390 mL
0.1952 mL
0.3903 mL
0.9758 mL
100 mM
0.0312 mL
0.1561 mL
0.3122 mL
0.7806 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Y-27632129830-38-2Y27632Y 27632OrganoidROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKantiepileptic effectadipose tissue-derived stem cellsADSCsInhibitorinhibitorinhibit
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