555555

Rho Kinase Inhibitor V

The Rho Kinase Inhibitor V, also referenced under CAS 1072906-02-5, controls the biological activity of Rho Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Rho Kinase Inhibitor V, N-(4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-carboxamide
• Empirical Formula (Hill Notation): C₁₈H₁₅N₃O₃
• CAS Number: 1072906-02-5
• Molecular Weight: 321.33
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light beige
• solubility: ethanol: 2 mg/mL; DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C18H15N3O3/c22-18(17-11-23-15-3-1-2-4-16(15)24-17)21-14-7-5-12(6-8-14)13-9-19-20-10-13/h1-10,17H,11H2,(H,19,20)(H,21,22)
• InChI key: MCQBNMPALTYSES-UHFFFAOYSA-N

Description

General description

A cell-permeable pyrazolyl carboxamide compound that acts as a potent, ATP-binding pocket-targeting inhibitor of ROCK-II (IC₅₀ = 1.5 nM) and effectively inhibits the myosin light chain 2 phosphorylation on Thr18/Ser19 in A7r5 cells (IC₅₀ = 72 nM). It afftects the activities of PKA, MRCK, Akt1 (IC₅₀ = 0.186, 1.19, and 1.41 µM, respectively) and CYP-450 enzymes (% inhibition of 2C9/2D6/3A4/1A2 at 10 µM = 87/40/1/20, respectively) only at much higher concentrations.

Feng, Y., et al. 2008. J. Med. Chem.51, 6642.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable