Tpl2 Kinase Inhibitor 1 hydrochloride
Based on 2 publication(s) in Google Scholar
Tpl2 Kinase Inhibitor 1 hydrochloride is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 hydrochloride plays an important role in the regulation of the inflammatory response and the progression of some cancers.
For research use only. We do not sell to patients.
- CAS No.: 2934185-09-6
- Formula: C21H15Cl2FN6
- Molecular Weight:441.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tpl2 Kinase Inhibitor 1 hydrochloride
MoreAll MAP3K Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
MAP3K8/COT/Tpl2 |
p38 180 μM (IC50) |
MK2 110 μM (IC50) |
In Vitro
Tpl2 (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family that is upstream of MEK in the ERK pathway[1].
Cancer Osaka thyroid (COT) kinase (Tpl2) is an important regulator of pro-inflammatory cytokines in macrophages[2].
Tpl2 Kinase Inhibitor 1 (compound 2p) hydrochloride also inhibits MK2 and p38, with IC50s of 110 μM and 180 μM, respectively in A431 cells[1].
Tpl2 Kinase Inhibitor 1 hydrochloride inhibits lipopolysaccharide-induced TNF-a production from primary human monocytes and human whole-blood, with IC50s of 0.7 μM and 8.5 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2934185-09-6
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Molecular Weight 441.29
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Formula C21H15Cl2FN6
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SMILES
FC1=CC=C(NC2=C(C=NC3=C2C=C(NCC4=CN=CC=C4)N=C3)C#N)C=C1Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Astragaloside Ⅳ negatively regulates Gpr97-TPL2 signaling to protect against hyperhomocysteine-exacerbated sepsis associated acute kidney injury. [Abstract]2024 Mar:125:155346. PMID: 38237511 -
Purity & Documentation
References
[1]. Gavrin LK, et al. Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92. [Content Brief]
[2]. Glatthar R, et al. Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J Med Chem. 2016 Aug 25;59(16):7544-60. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tpl2 Kinase Inhibitor 1 hydrochloride Related Classifications
HY-12358A Related Classifications
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