444965

MEK Inhibitor VIII

The MEK1/2 Inhibitor II, also referenced under CAS 212631-61-3, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): MEK Inhibitor VIII, N-Cyclopropylmethoxy-3,4,5-trifluoro-2-(4-iodo-2-methylphenylamino)benzamide
• Empirical Formula (Hill Notation): C₁₈H₁₆F₃IN₂O₂
• CAS Number: 212631-61-3
• Molecular Weight: 476.23
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 45 mg/mL; ethanol: 45 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C18H16F3IN2O2/c1-9-6-11(22)4-5-14(9)23-17-12(7-13(19)15(20)16(17)21)18(25)24-26-8-10-2-3-10/h4-7,10,23H,2-3,8H2,1H3,(H,24,25)
• InChI key: UHAXDAKQGVISBZ-UHFFFAOYSA-N

Description

General description

A cell-permeable and orally available amino-benzamide compound that acts as a potent and non-ATP-competitive inhibitor of MEK1/2 (IC₅₀ = 8 nM) with an excellent selectivity over ERK, c-Src, Cdk′s, and PI 3-Kγ (IC₅₀ >1.0 µM). Reported to exhibit in vivo efficacy in several animal models of arthritis and hyperalgesia in rat and rabbit.

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.

Other Notes

Pelletier, J.P., et al. 2003. Arthritis Rheum.48, 1582.
Ciruela, A., et al. 2003. Br. J. Pharmacol.138, 751.
Bhattachar, S.N., et al. 2002. Int. J. Pharm.236, 135.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable