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Merck
CN

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.

别名:

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

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关于此项目

经验公式（希尔记法）:
C17H13BrClF2IN2O2
化学文摘社编号:
212631-67-9
分子量:
557.56
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD16038897

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产品名称

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.

SMILES string

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

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 100 mg/mL
ethanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

相关类别

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

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.

Packaging

Packaged under inert gas

Preparation Note

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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