[CAS NO. 173897-44-4] Y-39983 HCl
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PRODUCTS SPECIFICATIONS [173897-44-4]
Store
Catalog
SLK-S7935
Brand
Selleck
CAS
173897-44-4
DESCRIPTION [173897-44-4]
Overview
| MDL | MFCD00945328 |
|---|---|
| Molecular Weight | 353.25 |
| Molecular Formula | C16H16N4O.2HCl |
| SMILES | O=C(NC1=C2C(NC=C2)=NC=C1)C3=CC=C([C@H](N)C)C=C3.[H]Cl.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8309 mL | 14.1543 mL | 28.3086 mL |
| 5 mM | 0.5662 mL | 2.8309 mL | 5.6617 mL |
| 10 mM | 0.2831 mL | 1.4154 mL | 2.8309 mL |
| 50 mM | 0.0566 mL | 0.2831 mL | 0.5662 mL |
Description
Y-39983 HCl (Y-33075) is a selective 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.
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.
References
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