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Merck
CN

444939

MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem

The MEK1/2 Inhibitor, also referenced under CAS 305350-87-2, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem, SL327, Z-& E-α-(Amino-((4-aminophenyl)thio)methylene)-2-(trifluoromethyl)benzeneacetonitrile

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关于此项目

经验公式（希尔记法）:
C16H12F3N3S
化学文摘社编号:
305350-87-2
分子量:
335.35
UNSPSC Code:
12352200
MDL number:
MFCD06411432

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assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

ethanol: 10 mg/mL, DMSO: 200 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

General description

A cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK1/2 (IC50 = 180 nM and 220 nM, respectively). Shown to inhibit AP-1 activity (IC50 = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities at higher concentrations (IC50 >10 µM). Reported to offer neuroprotection against ischemic brain injury in mice by selectively blocking ERK1/2 activation. Also suppresses IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Uncompetitive with respect to ATP.
A cell-permeable, vinylogous cyanamide that acts as a selective inhibitor of MEK1 (IC50 = 180 nM) and MEK2 (IC50 = 220 nM). Also shown to inhibit AP-1 activity (IC50 = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities only at higher concentrations (IC50 >10 µM). Reported to exhibit neuroprotective effects against ischemic brain injury in mice by selectively blocking ERK1/2 activation (i.e. noncompetitive with respect to ATP). Also reported to suppress IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Supplied as a mixture of Z- and E-isomers.
Supplied as a mixture of Z- and E-isomers.

Biochem/physiol Actions

Primary Target
MEK 1, MEK 2
Product does not compete with ATP.
Reversible: no
Target IC50: 180 nM and 220 nM against MEK1 and MEK2, respectively
Cell permeable: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Hetman, M., et al. 2002. J. Biol. Chem.277, 49577.
Ohno, M., et al. 2001. Nat. Neurosci.4, 1238.
Wang, H., et al. 2001. Biochem. Biophys. Res. Commun.286, 869.
Scherle, P.A., et al. 2000. J. Biol. Chem.275, 37086.
Valjent, E., et al. 2000. J. Neurosci.20, 8701.
Watabe, A.M., et al. 2000. J. Neurosci.20, 5924.
Atkins, C.M., et al. 1998. Nat. Neurosci.1, 602.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

法规信息

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相关内容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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