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ROCK inhibitor-2 [1127308-52-4]

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embalaje : 10mM/1mL

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ROCK inhibitor-2 | ROCK Inhibitor | MedChemExpress

ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC₅₀ values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC₅₀ of 75 nM. ROCK inhibitor-2 exhibits antitumor activity.

Para uso exclusivo en investigación. No vendemos a pacientes.

ROCK inhibitor-2 Estructura química

No. CAS : 1127308-52-4

Revisión del cliente

Based on 2 publication(s) in Google Scholar

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas ROCK:

Ver todas las isoformas

ROCK ROCK1 ROCK2

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target^[1]

ROCK1

160 nM (IC₅₀)

ROCK2

21 nM (IC₅₀)

In Vitro

ROCK inhibitor-2 (50 μM, 24-48 h) reduces the formation of cell-in-cell structure in cell U2OS, inhibits the cell migration and invasion of U2OS, and leads to mitochondrial dysfunction^[2].

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

Cell Migration Assay ^[2]

Cell Line:	U2OS
Concentration:	50 μM
Incubation Time:	48 h
Result:	Inhibited cell migration.

Western Blot Analysis^[2]

Cell Line:	U2OS
Concentration:	50 μM
Incubation Time:	24 h
Result:	Downregulated the expression of PGC1α, NRF1 and TFAM.

In Vivo

ROCK inhibitor-2 (10 mg/kg*day, ip, 27 days) exhibits antitumor efficacy in U2OS xenograft mouse models^[2].

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

Animal Model:	U2OS xenograft mouse models^[2]
Dosage:	10 mg/kg*day
Administration:	ip, 27 days
Result:	Inhibited tumor growth.

Peso molecular

332.40

Fòrmula

C₂₁H₂₀N₂O₂

No. CAS

1127308-52-4

Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@H](C)C1=CC=CC(OC)=C1)C(C=C2)=CC=C2C3=CC=NC=C3

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 200 mg/mL (601.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0084 mL	15.0421 mL	30.0842 mL
5 mM	0.6017 mL	3.0084 mL	6.0168 mL
10 mM	0.3008 mL	1.5042 mL	3.0084 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 5 mg/mL (15.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (15.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (15.04 mM); Clear solution

This protocol yields a clear solution of ≥ 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 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.92%

Select Batch:

Ficha de datos (281 KB) SDS (251 KB)

COA (245 KB) HNMR (259 KB) RP-HPLC (159 KB) LCMS (374 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Hobson AD, et al. Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based DrugDesign. J Med Chem. 2018 Dec 27;61(24):11074-11100. [Content Brief]

[2]. Zhang W, et al., 3D-printing magnesium-polycaprolactone loaded with melatonin inhibits the development of osteosarcoma by regulating cell-in-cell structures. J Nanobiotechnology. 2021 Sep 4;19(1):263. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0084 mL	15.0421 mL	30.0842 mL	75.2106 mL
	5 mM	0.6017 mL	3.0084 mL	6.0168 mL	15.0421 mL
	10 mM	0.3008 mL	1.5042 mL	3.0084 mL	7.5211 mL
	15 mM	0.2006 mL	1.0028 mL	2.0056 mL	5.0140 mL
	20 mM	0.1504 mL	0.7521 mL	1.5042 mL	3.7605 mL
	25 mM	0.1203 mL	0.6017 mL	1.2034 mL	3.0084 mL
	30 mM	0.1003 mL	0.5014 mL	1.0028 mL	2.5070 mL
	40 mM	0.0752 mL	0.3761 mL	0.7521 mL	1.8803 mL
	50 mM	0.0602 mL	0.3008 mL	0.6017 mL	1.5042 mL
	60 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2535 mL
	80 mM	0.0376 mL	0.1880 mL	0.3761 mL	0.9401 mL
	100 mM	0.0301 mL	0.1504 mL	0.3008 mL	0.7521 mL

ROCK inhibitor-2 Related Classifications

Help & FAQs

Keywords:

ROCK inhibitor-21127308-52-4ROCK inhibitor2ROCK inhibitor 2ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKpMYPT1Inhibitorinhibitorinhibit

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Nombre del producto:: ROCK inhibitor-2
Cat. No.:: HY-119937
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HY-119937-5mg

ROCK inhibitor-2 [1127308-52-4]

5mg

ROCK inhibitor-2 [1127308-52-4]

Referencia HY-119937-1ml

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

Revisión del cliente

ROCK inhibitor-2 Related Antibodies

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas ROCK:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

ROCK inhibitor-2 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

ROCK inhibitor-2 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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