Y-39983 is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
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
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Name | Y-39983 HCl |
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Iupac Chemical Name | Y-39983 HCl |
Synonyms | Y-33075 HCl |
Molecular Formula | C16H16N4O.2HCl |
Molecular Weight | 353.25 |
Smile | C[C@H](c1ccc(cc1)C(=O)Nc2ccnc3c2cc[nH]3)N.Cl.Cl |
InChiKey | CKFHAVRPVZNMGT-YQFADDPSSA-N |
InChi | InChI=1S/C16H16N4O.2ClH/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15;;/h2-10H,17H2,1H3,(H2,18,19,20,21);2*1H/t10-;;/m1../s1 |
CAS Number | 173897-44-4 |
MDL | MFCD00945328 |
Related CAS |
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Formulation | crystalline solid |
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Purity | 98% |
Storage | 3 years -20ºCpowder |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
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Clinical study |