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Y-39983 Dihydrochloride ROCK inhibitor

Name: Y-39983 Dihydrochloride
Brand: Selleck Chemicals
SKU: S7935
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S7935

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

Chemical Structure

Molecular Weight: 353.25

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP (HSP90) PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	353.25	Formula	C₁₆H₁₆N₄O.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	173897-44-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Y-33075 Dihydrochloride			Smiles	CC(C1=CC=C(C=C1)C(=O)NC2=C3C=CNC3=NC=C2)N.Cl.Cl

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.550mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 71 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.580mg/ml (1.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	ROCK ^[1] (Cell-free assay) 3.6 nM
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].
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].
References	https://pubmed.ncbi.nlm.nih.gov/26486225/ https://pubmed.ncbi.nlm.nih.gov/24008512/ https://pubmed.ncbi.nlm.nih.gov/21850162/