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Tpl2 Kinase Inhibitor (hydrochloride) (Synonyms: c-Cot Kinase Inhibitor, MAP3K8 Kinase Inhibitor, Tumor Progression Locus 2 Kinase Inhibitor)

Katalog-Nr.GC49150

A Tpl2 inhibitor

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Tpl2 Kinase Inhibitor (hydrochloride) Chemische Struktur

Cas No.: N/A

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1 mg
77,00 $
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5 mg
308,00 $
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10 mg
425,00 $
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25 mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50 = 0.05 µM).1 It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 µM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 µM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 µM.2 Tpl2 kinase inhibitor (5 µM) inhibits the proliferation of KG-1a leukemia cells.3

1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.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 D3Cell Cycle9(22)4542-4551(2010)

Chemical Properties

Cas No. N/A SDF
Überlieferungen c-Cot Kinase Inhibitor, MAP3K8 Kinase Inhibitor, Tumor Progression Locus 2 Kinase Inhibitor
Canonical SMILES FC(C(Cl)=C1)=CC=C1NC2=C(C#N)C=NC(C=N3)=C2C=C3NCC4=CN=CC=C4.Cl
Formula C21H14ClFN6·XHCl M.Wt 404.8
Löslichkeit DMF: slightly soluble,DMSO: slightly soluble Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.4704 mL 12.3518 mL 24.7036 mL
5 mM 0.4941 mL 2.4704 mL 4.9407 mL
10 mM 0.247 mL 1.2352 mL 2.4704 mL
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