GLPBio

SR-3677

Catalog No.: GC10722Purity:>99.50%
COASDSData Sheet
Rho Kinase (ROCK-II) inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

SR-3677
Cas No.: 1072959-67-1
10mM (in 1mL DMSO)In Stock
$79.00
1
5mgIn Stock
$45.00
1
10mgIn Stock
$72.00
1
50mgIn Stock
$230.00
1
100mgIn Stock
$396.00
1
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Citations

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Description

SR-3677 is a novel, potent and highly selective inhibitor of Rho Kinase (ROCK-II) with the IC50 value of ~0.3nM in enzyme and cell based assays [1].

SR-3677 has been reported to selectively inhibit the ROCK- II with the IC50 values of ~3nM, ~3nM, 56nM, 3.968μM,1.190μM and 7.491μM for ROCK-II,ppMLC, ROCK-I, PKA, MRCK and Akt1, respectively. In addition, SR-3677 has been shown several key binding elements that contribute to the high potency and selectivity in the docking assay. Furthermore, SR-3677 has been revealed to be efficacious in enhancing aqueous humor outflow and in target modulation in the pharmacology studies [1].

References:
[1] Feng Y1, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5. doi: 10.1021/jm800986w. Epub 2008 Oct 4.

Protocol

Kinase experiment:

Assays are performed using the STK2 kinase system from Cisbio. 5 μL mixture of a 1 μM STK2 substrate and ATP (ROCK-I: 4 μM; ROCK-II: 20 μM) in STK-buffer is added to the wells. 20 nL of test compounds (SR-3677) is dispensed. Reaction is started by addition of 5 μL of 2.5 nM. ROCK-I or 0.5 nM ROCK-II in STK-buffer. After 4 h at RT the reaction is stopped by addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in detection buffer[1].

References:

[1]. Feng Y, et al. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1072959-67-1
Chemical Name
N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide
SMILES
CN(C)CCOC1=C(C=CC(=C1)C2=CNN=C2)NC(=O)C3COC4=CC=CC=C4O3
Molecular Formula
C22H24N4O4
Molecular Weight
408.45
Solubility
DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 5 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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