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ITRI-E-(S)4046

Chemical Structure : ITRI-E-(S)4046

CAS No.: 2661229-35-0

ITRI-E-(S)4046 (E(S)4046)

Catalog No.: PC-21300Not For Human Use, Lab Use Only.

ITRI-E-(S)4046 (E(S)4046) is a potent, highly specific, dual synergistic inhibitor of myosin light chain kinase 4 (MYLK4) and Rho-related protein kinase (ROCK) with IC50 of 3.2 nM and 25.6 nM for ROCK1 and MYLK4, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ITRI-E-(S)4046 (E(S)4046) is a potent, highly specific, dual synergistic inhibitor of myosin light chain kinase 4 (MYLK4) and Rho-related protein kinase (ROCK) with IC50 of 3.2 nM and 25.6 nM for ROCK1 and MYLK4, respectively.
ITRI-E-(S)4046 potently inhibits myosin light chain (MLC) phosphorylation (pMLC) with IC50 of 50.4 nM in HTM cells.
ITRI-E-(S)4046 exhibits a selective kinase inhibition profile targeting on the AGC kinase subfamily, and MYLK4, shows high specificity against protein kinase A, G, and C families.
ITRI-E-(S)4046 can reduceintraocular pressure (IOP) in normotensive and hypertensive animal models.

Physicochemical Properties

M.Wt 306.37
Formula C18H18N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(4-(1H-pyrazol-4-yl)phenyl)-3-amino-2-phenylpropanamide

References

1. Yi-Hsun Chen, et al. Invest Ophthalmol Vis Sci. 2021 Oct 4;62(13):12.

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