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Signal Inhibitors and Activators

TAK-733

$816/ 5mg
Quantity
Total: $816

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Product Information

Kinase Inhibitor Name TAK-733
FormulaC17H15F2IN4O4
SolubilityDMSO ≥101 mg/mL   Water <1 mg/mL   Ethanol <1 mg/mL
Stability:
2 years       -20℃     Powder
1 week        -4℃     in DMSO
1 month     -80℃     in DMSO
CAS No.1035555-63-5
Biological ActivityTAK-733 is highly potent and selective novel MEK allosteric site inhibitor with an IC50 of 3.2 nM. TAK-733 selectively binds to and inhibits the activity of MEK1/2. Subseqently, TAK-733 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often up-regulated in a variety of tumor cell types. TAK-733 has potent anticancer activity in various mouse xenograft models. TAK-733 showed potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. [1][2]
M.W.504.23
ReferencesDiscovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Dong Q et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9
MEK inhibitor TAK-733 http://cn.termwiki.com/EN:MEK_inhibitor_TAK-733
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Price816$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
highly potent and selective novel MEK allosteric site inhibitor with an binds to and inhibits the activity of MEK1/2. Subseqently, TAK-733 MEK1/2-dependent effector proteins and transcription factors, which may factor-mediated cell signaling and tumor cell proliferation. MEK1/2 threonine/tyrosine kinases that play key roles in the activation of the often up-regulated in a variety of tumor cell types. TAK-733 has potent
highly potent and selective novel MEK allosteric site inhibitor with an binds to and inhibits the activity of MEK1/2. Subseqently, TAK-733 MEK1/2-dependent effector proteins and transcription factors, which may factor-mediated cell signaling and tumor cell proliferation. MEK1/2 threonine/tyrosine kinases that play key roles in the activation of the often up-regulated in a variety of tumor cell types. TAK-733 has potent