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555550

Rho Kinase Inhibitor

The Rho kinase inhibitor, CAS 872543-07-6, is a cell-permeable, highly specific, reversible, potent, and ATP-competitive inhibitor of Rho-associated kinase (ROCK; Ki = 1.6 nM).

Synonyme(s) :

Rho Kinase Inhibitor, H-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)

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A propos de cet article

Formule empirique (notation de Hill) :
C16H21N3O2S · 2HCl
Numéro CAS:
871543-07-6
Poids moléculaire :
392.34
MDL number:
MFCD06411451
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

white

solubility

methanol: 5 mg/mL, water: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

[S](=O)(=O)(N3[C@H](CNCCC3)C)c1c2c(cncc2C)ccc1.Cl.Cl

InChI

1S/C16H21N3O2S.2ClH/c1-12-9-18-11-14-5-3-6-15(16(12)14)22(20,21)19-8-4-7-17-10-13(19)2;;/h3,5-6,9,11,13,17H,4,7-8,10H2,1-2H3;2*1H/t13-;;/m0../s1

InChI key

BFOPDSJOLUQULZ-GXKRWWSZSA-N

General description

A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27 μM for PKC, and 10.1 μM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H2O is also available.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
ROCK
Product competes with ATP.
Reversible: yes
Target Ki: 1.6 nM against G-protein Rho-associated kinase

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wen, Qiang, et al. 2012. Cell150, 575.
Ikenoya, M., et al. 2002. J. Neurochem.81, 9.
Sasaki, Y., et al. 2002. Pharmacol. Ther.93, 225.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Harmful (C)

Classe de stockage

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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