Potent and selective Tpl2 (Cot; MAP3K8) inhibitor (IC50 = 50 nM). Selective for Tpl2 over MEK, p38, Src, MK2, PKC and EGFR. Inhibits LPS-induced TNF-α secretion from monocytes and attenuates acute myeloid leukemia (AML) cell proliferation in vitro. Also reduces cytolytic activity of human CD8+ cytotoxic T lymphocytes. Cell permeable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 404.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.47 mL||12.35 mL||24.7 mL|
|5 mM||0.49 mL||2.47 mL||4.94 mL|
|10 mM||0.25 mL||1.24 mL||2.47 mL|
|50 mM||0.05 mL||0.25 mL||0.49 mL|
References are publications that support the biological activity of the product.
Chowdhury et al (2014) Pharmacological inhibition of TPL2/MAP3K8 blocks human cytotoxic T lymphocyte effector functions. PLoS ONE 9 e92187 PMID: 24642963
Wang et al (2010) Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3. Cell Cycle 9 4542 PMID: 21084834
Gavrin et al (2005) Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg.Med.Chem.Lett. 15 5288 PMID: 16165349
If you know of a relevant reference for TC-S 7006, please let us know.
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Keywords: TC-S 7006, TC-S 7006 supplier, TC-S7006, potent, selective, TPL2, Cot, MAP3K8, inhibits, inhibitors, Other, Kinases, 5240, Tocris Bioscience
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