Biological Activity
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.
Compound Libraries
TC-S 7006 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 404.83 |
| Formula | C21H14ClFN6 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 871307-18-5 |
| PubChem ID | 9549300 |
| InChI Key | NMEUKWOOQOHUNA-UHFFFAOYSA-N |
| Smiles | FC(C(Cl)=C4)=CC=C4NC1=C2C(C=NC(NCC3=CN=CC=C3)=C2)=NC=C1C#N |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.48 | 100 |
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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: TC-S 7006, supplier, TC-S7006, potent, selective, TPL2, Cot, MAP3K8, inhibits, inhibitors, Other, Kinases, Other, Kinases, Tocris Bioscience
