MEK1/2 Inhibitor IV-CAS 212631-67-9-Calbiochem

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一般描述

A cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC₅₀= 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC₅₀>10 M). Shown to be superior to PD 98059 and U0126 in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC₅₀<0.1 M)in vitroand effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED₅₀<50 mg/kg, i.p.)in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.
A cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC₅₀= 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC₅₀>10 ?M). Shown to be superior to PD 98059 (Cat. Nos. 513000 and 513001 and U0126 (Cat. No. 662005) in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC₅₀<0.1 ?M)in vitroand effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED₅₀<50 mg/kg, i.p.)in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

Yip-Schneider, M.T., et al. 2009.J. Pharmacol. Exp. Ther.329,1063.
Duman, C.H., et al. 2007.Biol. Psychiatry61,661.
Klein, P.J., et al. 2006.Neoplasia8,1.
Thottassery, J.V., et al. 2004.Cancer Res.64,4637.
Yung, H.W., et al. 2004.Biochem. Pharmacol.68,351.

法律信息

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

基本信息

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