Y-39983 HCl

Catalog No.S7935 Synonyms: Y-33075 HCl

Y-39983 HCl Chemical Structure

Molecular Weight(MW): 353.25

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

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Biological Activity

Description Y-39983 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

Cell Research:[3]
+ Expand
  • 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) supplemented with 10% fetal bovine serum and 10 μg/ml of gentamicin. 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: SJL/J mice
  • Formulation: Saline
  • Dosages: 100 μl of 10 μM
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (178.34 mM)
Water 63 mg/mL (178.34 mM)
Ethanol 2 mg/mL (5.66 mM)

* 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.

Chemical Information

Molecular Weight 353.25
Formula

C16H16N4O.2HCl

CAS No. 173897-44-4
Storage powder
Synonyms Y-33075 HCl

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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.

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ROCK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID