Y-39983 HCl

Catalog No.S7935 Synonyms: Y-33075 HCl

For research use only.

Y-39983 HCl (Y-33075) is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.

Y-39983 HCl Chemical Structure

CAS No. 173897-44-4

Selleck's Y-39983 HCl has been cited by 3 Publications

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Biological Activity

Description Y-39983 HCl (Y-33075) 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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TM1 MkfBSpVv[3Srb36gZZN{[Xl? MWLEbZNzfXC2aX;uJI9nKHS{YXLlZ5Vt[XJibXXzbJdwemtiaX6gbJVu[W5iVF2xJINmdGy|IHHzd4V{e2WmIHHzJIFkfGmwIH\pZoVzKGynbnf0bEBidmRiZn;jZYwh[WSqZYPpc45{KGK7IFjv[YNpe3Ric4ThbY5qdmdiYnHz[YQh[W6jbInzbZMtKEmFNUCgQUAxNjJ5ODFOwG0v MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5MkmwOUc,OjdyN{K5NFU9N2F-
GTM3 Ml[5SpVv[3Srb36gZZN{[Xl? NF\DcoYzKGSjeYO= MlP0TY5pcWKrdHnvckBw\iCUT1PLMVIhcW5iaIXtZY4hT1SPMzDj[YxteyCvZXHzeZJm\CC3cDD0c{AzKGSjeYOgZpkh[2WubDDpcZBm\GGwY3WgZZN{[XluIFXDOVAhRSByLkG1JO69VS5? M3jkU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nki0PFQ{Lz5{NE[4OFg1OzxxYU6=
GTM3 MXHGeY5kfGmxbjDhd5NigQ>? NGjSOZFKdmirYnn0bY9vKG:oIGLPR2syKGmwIHj1cYFvKEeWTUOgZ4VtdHNiYomgbY1x\WSjbnPlJIF{e2G7LDDFR|UxKD1iMD63PUDPxE1w MlLBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2M{SzN|QoRjJyNEO0N|M1RC:jPh?=
SJ-GBM2 NYHZe5dmeUiWUzDhd5NigQ>? MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= NVr2bm9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NIfEWFdyUFSVIHHzd4F6 M4[3fpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| M3f6RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC M3Wy[pFJXFNiYYPzZZk> NEO0RnhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MlHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MWHxTHRUKGG|c3H5 MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NIDpTZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MUXxTHRUKGG|c3H5 MlfrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NVTRVmJWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NYOwSoJSeUiWUzDhd5NigQ>? NY[5S5JueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot p-MYPT1 / ppMLC 21850162
Immunofluorescence F-actin / ppMLC 21850162
Growth inhibition assay Cell viability 27487152
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 Research:[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) 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.
Animal Research:[2]
  • Animal Models: SJL/J mice
  • Dosages: 100 μl of 10 μM
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 353.25
Formula

C16H16N4O.2HCl

CAS No. 173897-44-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=C(C=C1)C(=O)NC2=C3C=CNC3=NC=C2)N.Cl.Cl

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Tech Support

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