Y-27632 [146986-50-7]

Referência HY-10071-5mg

Tamanho : 5mg

Marca : MedChemExpress

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Description

Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade[1][2][3][4][5][6].

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)

Cellular Effect
Cell Line Type Value Description References
A7R5 EC50
200 nM
Compound: Y-27632
Inhibition of ROCK in rat A7r5 cells assessed as inhibition of MLC phosphorylation by direct ELISA
Inhibition of ROCK in rat A7r5 cells assessed as inhibition of MLC phosphorylation by direct ELISA
[PMID: 24119557]
A7R5 EC50
630 nM
Compound: Y-27632
Inhibition of ROCK-catalysed MLC Thr18/Ser19 phosphorylation in rat A7r5 cells after 90 mins by ELISA
Inhibition of ROCK-catalysed MLC Thr18/Ser19 phosphorylation in rat A7r5 cells after 90 mins by ELISA
[PMID: 25898023]
HEK293 IC50
600 nM
Compound: Y 27632
Inhibition of His-tagged human PRK2 expressed in HEK293 cells
Inhibition of His-tagged human PRK2 expressed in HEK293 cells
[PMID: 10998351]
PC-3 IC50
28 μM
Compound: Y-27632
Antimetastatic activity against human PC3 cells after 24 hrs by scratch wound assay
Antimetastatic activity against human PC3 cells after 24 hrs by scratch wound assay
[PMID: 23707258]
Sf9 IC50
150 nM
Compound: Y-27632
Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
[PMID: 17018693]
Sf9 IC50
8.3 μM
Compound: Y 27632
Inhibition of His-tagged human MSK1 expressed in Sf9 cells
Inhibition of His-tagged human MSK1 expressed in Sf9 cells
[PMID: 10998351]
Sf9 IC50
800 nM
Compound: Y 27632
Inhibition of rat ROCK2 expressed in Sf9 cells
Inhibition of rat ROCK2 expressed in Sf9 cells
[PMID: 10998351]
In Vitro

Y-27632 (10 μM; 24-72 h) significantly reduces the viability of CAL-27, SCC-4 and SCC-9 oral squamous cell carcinoma (OSCC) cells[2].
Y-27632 (10 μM; 24 h) significantly inhibits the migration of CAL-27, SCC-4 and SCC-9 cells[2].
Y-27632 (10 μM; 6-24 h) inactivates the AKT/mTOR pathway, reduces the levels of phosphorylated downstream effectors, and increases the levels of apoptosis markers in OSCC cells[2].
Y-27632 (10 μM) induces autophagy in OSCC cells by inhibiting the mTOR pathway and promoting the conversion of LC3-I to LC3-II[2].
Y-27632 (10-50 μM; 5 min-3 h) induces dose- and time-dependent neurite outgrowth in PC12 cells via the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade[4].
Y-27632 (10-1000 μM; 24 h) dose-dependently promotes the formation of F-actin/tubulin-containing Y-NTs (average length 30 μm) in ARPE19 retinal pigment epithelial cells and increases the mitochondrial transfer rate; this effect also exists under photodamage conditions, and mitochondrial transfer depends on direct contact between cells[5].
Y-27632 (40 μM; 24 h) induces cytoskeleton remodeling and morphological changes (increased cell area, enhanced contour length and pseudopodium formation) in ARPE19 retinal pigment epithelial cells, without altering the protein expression of F-actin or α-tubulin[5].
Y-27632 (40 μM; 24 h) alters mitochondrial distribution to an infiltrative and axon-like pattern, enhances mitochondrial mobility, upregulates miro1 mRNA expression, and increases the number and length of individual mitochondria in ARPE19 retinal pigment epithelial cells[5].
Y-27632 (10-1000 μM; 24 h) reduces the viability and promotes the apoptosis of ARPE19 retinal pigment epithelial cells only when the concentration exceeds 40 μM, and exerts no significant effects at concentrations of 10 μM, 20 μM or 40 μM[5].
Y-27632 (40 μM; 24 h) induces Y-shaped nanotubes (Y-NTs) in ARPE19 retinal pigment epithelial cells, a process that depends primarily on F-actin; in contrast, Y-27632-enhanced mitochondrial transport via Y-NTs relies on both F-actin and microtubules[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (202.15 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2 mg/mL (8.09 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0430 mL 20.2151 mL 40.4302 mL
5 mM 0.8086 mL 4.0430 mL 8.0860 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 (protect from light, stored under nitrogen). 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.

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.11 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 μL DMSO 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 (10.11 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 μL DMSO 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.

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:  Saline

    Solubility: 2 mg/mL (8.09 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

Pureté et documentation
Références

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Referência
Descrição
Cond.
Price Bef. VAT
0863-SC
 5ml 
331-22252-3
 10mg 
144-07334-100
 100uL