Y-39983 Dihydrochloride

Catalog No.S7935 Batch:S793504

Technical Data

Formula

C₁₆H₁₆N₄O.2HCl

Molecular Weight

353.25

CAS No.

173897-44-4

Solubility (25°C)*

In vitro

DMSO

70 mg/mL (198.15 mM)

Water

70 mg/mL (198.15 mM)

Ethanol

2 mg/mL (5.66 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.58mg/ml	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.55mg/ml	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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].

Protocol (from reference)

Cell Assay:^{^[3]}	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.
Animal Study:^{^[2]}	Animal Models SJL/J mice Dosages 100 μl of 10 μM Administration i.p.

Cell Assay:^{^[3]}

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.

Animal Study:^{^[2]}

Animal Models
SJL/J mice
Dosages
100 μl of 10 μM
Administration
i.p.

References

Selleck's Y-39983 Dihydrochloride has been cited by 5 publications

Effects of Rho-Associated Kinase (Rock) Inhibitors (Alternative to Y-27632) on Primary Human Corneal Endothelial Cells [ Cells, 2023, 12(9)1307]	PubMed: 37174707
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325
Simulated microgravity inhibits the viability and migration of glioma via FAK/RhoA/Rock and FAK/Nek2 signaling. [ In Vitro Cell Dev Biol Anim, 2019, 55(4):260-271]	PubMed: 30820814
Phosphorylation of ARHGAP19 by CDK1 and ROCK regulates its subcellular localization and function during mitosis. [ J Cell Sci, 2018, 131(5)]	PubMed: 29420299

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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