616373
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.
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所有图片(1)
别名:
Tpl2 Kinase Inhibitor, 4-(3-Chloro-4-fluorophenylamino)-6-(pyridin-3-yl-methylamino)-3-cyano-[1,7]-naphthyridine
经验公式（希尔记法）:
C21H14ClFN6
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质量水平
检测方案
≥95% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
−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
一般描述
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).
生化/生理作用
Cell permeable: yes
Primary Target
Tpl2 Kinase
Tpl2 Kinase
Product competes with ATP.
Reversible: yes
Target IC50: 50 nM against Tpl2 kinase
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Gavrin, L.K., et al. 2005. Bioorg. Med. Chem. Lett.15, 5288.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2
WGK
WGK 2
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)
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
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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