444967

MEK1/2 Inhibitor IV

The MEK1/2 Inhibitor IV, also referenced under CAS 212631-67-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: MEK1/2 Inhibitor IV, 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV, MEK Inhibitor IV, 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161
• 実験式（ヒル表記法）: C₁₇H₁₃BrClF₂IN₂O₂
• CAS番号: 212631-67-9
• 分子量: 557.56
• MDL番号: MFCD16038897
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mg/mL; ethanol: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: Ic1cc(c(cc1)Nc2c(c(c(cc2C(=O)NOCC3CC3)Br)F)F)Cl
• InChI: 1S/C17H13BrClF2IN2O2/c18-11-6-10(17(25)24-26-7-8-1-2-8)16(15(21)14(11)20)23-13-4-3-9(22)5-12(13)19/h3-6,8,23H,1-2,7H2,(H,24,25)
• InChI Key: VJNZMSLGVUSPCF-UHFFFAOYSA-N

詳細

詳細

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 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.

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable