Tpl2 Kinase InhibitorA reversible competitive inhibitor of Tpl2 kinase

Tpl2 Kinase Inhibitor (CAS 871307-18-5)

Tpl2 Kinase Inhibitor | CAS 871307-18-5 is rated 5.0 out of 5 by 1.
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Synonym: 4-(3-Chloro-4-fluorophenylamino)-6-(pyridin-3-yl-methylamino)-3-cyano-[1,7]-naphthyridine
Application: A reversible competitive inhibitor of Tpl2 kinase
CAS Number: 871307-18-5
Purity: ≥95%
Molecular Weight: 404.83
Molecular Formula: C21H14ClFN6
* Refer to Certificate of Analysis for lot specific data (including water content).
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Tpl2 Kinase Inhibitor is a reversible naphthyridine ATP-competitive inhibitor of the enzyme Cot (Tpl2 kinase). The enzyme is a hematopoietically expressed serine-threonine kinase responsible for regulating tumor necrosis factor-α, toll-like receptor, and G protein–coupled receptor signaling. Studies suggest that Cot (Tpl2 kinase) inhibitor suppresses LPS-induced (sc-3535) TNF-α production from primary human monocytes. In addition, Tpl2 kinase inhibitor causes an increase in 1,25-Dihydroxyvitamin D3 (1,25D)-induced differentiation of myeloid leukemia cells via inhibition of Cot (Tpl2 kinase).


References

1. Watford, W.T., et al. 2008. J. Exp. Med. 205: 2803-2812. PMID: 19001140
2. Wang, X., et al. 2010. Cell Cycle. 9: 4542-4551. PMID: 21084834
3. Wang, X., et al. 2010. J. Steroid Biochem. Mol. Biol. 121: 395-398. PMID: 20227498

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml).
Storage :
Store at -20° C
Melting Point :
240.54° C (Predicted)
Boiling Point :
616.32° C at 760 mmHg (Predicted)
Density :
1.46 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
Tpl2 kinase: IC50 = 50 nM; EGFR: IC50 = 5 µM; MEK,: IC50 = >40 µM; MK2: IC50 = 110 µM; p38: IC50 = 180 µM
pK Values :
pKb: 4.8 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9549300
SMILES :
C1=CC(=CN=C1)CNC2=NC=C3C(=C2)C(=C(C=N3)C#N)NC4=CC(=C(C=C4)F)Cl

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Certificate of Analysis

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Tpl2 Kinase Inhibitor  Product Citations

See how others have used Tpl2 Kinase Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 31444264  Piersma, SJ.|Pak-Wittel, MA.|Lin, A.|Plougastel-Douglas, B.|Yokoyama, WM.| et al. 2019. J. Immunol.

PMID: # 30617349  Choi, Y.|Park, SJ.|Sun, Y.|Yoo, JS.|Pudupakam, RS.|Foo, SS.|Shin, WJ.|Chen, SB.|Tsichlis, PN.|Lee, WJ.|Lee, JS.|Li, W.|Brennan, B.|Choi, YK.|Jung, JU.| et al. 2019. Nat Microbiol.

PMID: # 29844241  Wang, Y.|Wang, S.|Kelly, CP.|Feng, H.|Greenberg, A.|Sun, X.| et al. 2018. Infect. Immun. 86:

PMID: # 26999821  Sharma, V.|Young, L.|Cavadas, M.|Owen, K.|, .| et al. 2016. Elife. 5:

PMID: # 24642963  Chowdhury, FZ. et al. 2014. PloS one. 9: e92187.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Kaniaris Kaniaris, E. et al. (PubMed 26266915) found that WT mice treated with the Tpl2 Kinase Inhibitor, either prior of after the initiation of high tidal volume ventilation were protected from the development of lung injury, as indicated by preserved lung compliance and lower BALF concentrations of proteins and IL-6, than similarly ventilated, untreated wild-type mice. -SCBT Publication Review
Date published: 2015-07-01
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