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MEK1/2 Inhibitor IV
2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV
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 µM). 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 µM) in vitro and 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.
产品信息
Form White solid
Molar mass 557.6
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO or EtOH
Chemical formula C17H13BrClF2IN2O2
CAS number 212631-67-9
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |