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Submit ReviewTC-S 7006 is a 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.
TC-S 7006 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 404.83 |
公式 | C21H14ClFN6 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.48 | 100 |
以下数据基于产品分子量 404.83。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: TC-S 7006, TC-S 7006 supplier, TC-S7006, potent, selective, TPL2, Cot, MAP3K8, inhibits, inhibitors, Other, Kinases, 5240, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TC-S 7006 的部分引用包括:
Matzaraki et al (2017) An integrative genomics approach identifies novel pathways that influence candidaemia susceptibility. PLoS One 12 e0180824 PMID: 28727728
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