Information Y-39983 HCl Y-39983 HCl (Y-33075) is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM. Targets ROCK (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. Cell Research(from reference) Cell lines：Human glaucomatous trabecular meshwork (GTM3) cell line Concentrations：5 μM Incubation Time：1 h
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Y-39983 HCl
CAS number：173897-44-4 molecular formula：C16H18Cl2N4O
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| Chinese alias | - | ||
| English alias | 4-[(1R)-1-Aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide--hydrogen chloride (1/2) | SCHEMBL599800 | BS-49924 | A921358 | 4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide;dihydrochloride | HY-10069 | Y-33075 2HCl | Y-39983 dihydroch | ||
| CAS number | 173897-44-4 | molecular formula | C16H18Cl2N4O |
| molecular weight | 353.25 g/mol | Exact mass | ≥97% |
| PSA | 83.800 Ų | logp | - |
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