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616373

Sigma-Aldrich

Tpl2 Kinase Inhibitor

The Tpl2 Kinase Inhibitor, also referenced under CAS 871307-18-5, controls the biological activity of Tpl2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Tpl2 Kinase Inhibitor, 4-(3-Chloro-4-fluorophenylamino)-6-(pyridin-3-yl-methylamino)-3-cyano-[1,7]-naphthyridine

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About This Item

Empirical Formula (Hill Notation):
C21H14ClFN6
CAS Number:
871307-18-5
Molecular Weight:
404.83
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C21H14ClFN6/c22-17-6-15(3-4-18(17)23)29-21-14(8-24)11-26-19-12-28-20(7-16(19)21)27-10-13-2-1-5-25-9-13/h1-7,9,11-12H,10H2,(H,26,29)(H,27,28)

InChI key

NMEUKWOOQOHUNA-UHFFFAOYSA-N

General description

A cell-permeable naphthyridine compound that acts as a potent, reversible, and ATP-competitive inhibitor of Tpl2 kinase (IC50 = 50 nM). Displays significant selectivity over other related kinases (IC50 = 5, >40, 110, 180, >400 and >400 µM for EGFR, MEK, MK2, p38, Src, and PKC, respectively). Shown to inhibit LPS-induced TNF-α production both from primary human monocytes and in whole blood (IC50 = 700 nM and 8.5 µM, respectively).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Tpl2 Kinase
Product competes with ATP.
Reversible: yes
Target IC50: 50 nM against Tpl2 kinase

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Gavrin, L.K., et al. 2005. Bioorg. Med. Chem. Lett.15, 5288.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H315,H319

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Cory M Johannessen et al.
Nature, 468(7326), 968-972 (2010-11-26)
Oncogenic mutations in the serine/threonine kinase B-RAF (also known as BRAF) are found in 50-70% of malignant melanomas. Pre-clinical studies have demonstrated that the B-RAF(V600E) mutation predicts a dependency on the mitogen-activated protein kinase (MAPK) signalling cascade in melanoma-an observation
Kara D Wyatt et al.
PloS one, 17(1), e0262832-e0262832 (2022-01-21)
Tumor progression locus 2 (Tpl2) is a serine/threonine kinase that regulates the expression of inflammatory mediators in response to Toll-like receptors (TLR) and cytokine receptors. Global ablation of Tpl2 leads to severe disease in response to influenza A virus (IAV)
Aikaterini Nanou et al.
Cell reports, 35(8), 109168-109168 (2021-05-27)
Increased vascular permeability and leakage are hallmarks of several pathologies and determine disease progression and severity by facilitating inflammatory/metastatic cell infiltration. Using tissue-specific genetic ablation in endothelial cells, we have investigated in vivo the role of Tumor progression locus 2 (Tpl2)
Timothy M Errington et al.
eLife, 10 (2021-12-08)
As part of the Reproducibility Project: Cancer Biology, we published Registered Reports that described how we intended to replicate selected experiments from 29 high-impact preclinical cancer biology papers published between 2010 and 2012. Replication experiments were completed and Replication Studies

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