Home Cell Cycle ROCK inhibitor Y-39983 Dihydrochloride For research use only.

Y-39983 Dihydrochloride

Synonyms: Y-33075 Dihydrochloride

Y-39983 (Y-33075)Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.

Y-39983 Dihydrochloride Chemical Structure

Y-39983 Dihydrochloride Chemical Structure

CAS No. 173897-44-4

Purity & Quality Control

Y-39983 Dihydrochloride Related Products

Signaling Pathway

ROCK Signaling Pathways

ROCK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TM1 Function assay Disruption of trabecular meshwork in human TM1 cells assessed as actin fiber length and focal adhesions by Hoechst staining based analysis, IC50 = 0.278 μM. 27072905
GTM3 Function assay 2 days Inhibition of ROCK-2 in human GTM3 cells measured up to 2 days by cell impedance assay, EC50 = 0.15 μM. 24684843
GTM3 Function assay Inhibition of ROCK1 in human GTM3 cells by impedance assay, EC50 = 0.79 μM. 20434334
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Y-39983 (Y-33075)Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
Targets
ROCK [1]
(Cell-free assay)
3.6 nM
In vitro
In vitro

Y-39983 opposes ROCK-dependent phosphorylation of MYPT1 predominantly at Thr853 with a corresponding decrease in MLC phosphorylation. It reduces the phosphorylation at Thr696 and Thr853 and leads to reduced actomyosin contraction. Y-39983 shows an IC50 of ~200 nM for dephosphorylation at Thr696 and only 15 nM for dephosphorylation at Thr853. The IC50 for dephosphorylation of MLC is 14 nM[3].
Cell Research Cell lines Human glaucomatous trabecular meshwork (GTM3) cell line
Concentrations 5 μM
Incubation Time 1 h
Method

Cell cultures of an immortalized human glaucomatous trabecular meshwork (GTM3) cell line are grown at 37℃ in 5% CO2 in Dulbecco's Minimum Essential Medium (DMEM + Glutamax) . Upon reaching confluence, cells are divided using 0.05% trypsin. Cells of passages 13 to 20 are used in experiments. Cells are treated with 5 μM of the specific ROCK inhibitors, Y-27632 and Y-39983, for 1 h in a serum-rich medium. Cell lysate is used for western blotting to test effect of ROCK inhibitors on the phosphorylation of MYPT1 and MLC.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-MYPT1 / ppMLC 21850162
Immunofluorescence F-actin / ppMLC 21850162
Growth inhibition assay Cell viability 27487152
In Vivo
In vivo

Y-39983 significantly suppresses clinical symptoms of EAE and prevents its relapse while increasing the amount of myelin proteins. Its treatment results in reduced demyelination with no significant change in axonal damage, which may be due to the inactivation of ROCK substrates, including phosphorylated (p)-MLC, LIMK2 and CRMP-2, which are important for neurite outgrowth, growth cone collapse and remyelination of oligodendrocytes[2].
Animal Research Animal Models SJL/J mice
Dosages 100 μl of 10 μM
Administration i.p.

Chemical Information & Solubility

Molecular Weight 353.25 Formula

C16H16N4O.2HCl
CAS No. 173897-44-4 SDF Download Y-39983 Dihydrochloride SDF
Smiles CC(C1=CC=C(C=C1)C(=O)NC2=C3C=CNC3=NC=C2)N.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (178.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 63 mg/mL

Ethanol : 2 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Y-39983 Dihydrochloride | Y-39983 Dihydrochloride supplier | purchase Y-39983 Dihydrochloride | Y-39983 Dihydrochloride cost | Y-39983 Dihydrochloride manufacturer | order Y-39983 Dihydrochloride | Y-39983 Dihydrochloride distributor