Cat. No.: HY-12358

Tpl2 Kinase Inhibitor 1

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Tpl2 Kinase Inhibitor 1 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 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.

Purity: 99.42%
CAS No.: 871307-18-5
Formula: C₂₁H₁₄ClFN₆
Molecular Weight:404.83

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tpl2 Kinase Inhibitor 1 Chemical Structure

CAS No.: 871307-18-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

MAP3K8/COT/Tpl2

p38

180 μM (IC₅₀)

MK2

110 μM (IC₅₀)

All MAP3K Isoforms :

All p38 MAPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	<5 μM Compound: 1b	Inhibition of EGFR kinase autophosphorylation in A431 cells Inhibition of EGFR kinase autophosphorylation in A431 cells	[PMID: 17664070]
Monocyte	IC₅₀	1.1 μM Compound: 1b	Inhibition of LPS-induced TNFalpha production in human monocytes Inhibition of LPS-induced TNFalpha production in human monocytes	[PMID: 17664070]

In Vitro

Tpl2 (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family that is upstream of MEK in the ERK pathway^[1].
Tpl2 Kinase Inhibitor 1 (compound 2p) also inhibits MK2 and p38, with IC₅₀s of 110 μM and 180 μM, respectively in A431 cells^[1].
Tpl2 Kinase Inhibitor 1 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].
Cancer Osaka thyroid (COT) kinase (Tpl2) is an important regulator of pro-inflammatory cytokines in macrophages^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 871307-18-5
Appearance Solid
Molecular Weight 404.83
Formula C₂₁H₁₄ClFN₆
Color Yellow to green
SMILES

N#CC1=C(NC2=CC=C(F)C(Cl)=C2)C3=CC(NCC4=CC=CN=C4)=NC=C3N=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (247.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4702 mL

12.3509 mL

24.7017 mL

5 mM

0.4940 mL

2.4702 mL

4.9403 mL

10 mM

0.2470 mL

1.2351 mL

2.4702 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4702 mL	12.3509 mL	24.7017 mL	61.7543 mL
	5 mM	0.4940 mL	2.4702 mL	4.9403 mL	12.3509 mL
	10 mM	0.2470 mL	1.2351 mL	2.4702 mL	6.1754 mL
	15 mM	0.1647 mL	0.8234 mL	1.6468 mL	4.1170 mL
	20 mM	0.1235 mL	0.6175 mL	1.2351 mL	3.0877 mL
	25 mM	0.0988 mL	0.4940 mL	0.9881 mL	2.4702 mL
	30 mM	0.0823 mL	0.4117 mL	0.8234 mL	2.0585 mL
	40 mM	0.0618 mL	0.3088 mL	0.6175 mL	1.5439 mL
	50 mM	0.0494 mL	0.2470 mL	0.4940 mL	1.2351 mL
	60 mM	0.0412 mL	0.2058 mL	0.4117 mL	1.0292 mL
	80 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7719 mL
	100 mM	0.0247 mL	0.1235 mL	0.2470 mL	0.6175 mL

Keywords

Tpl2 Kinase Inhibitor 1

1 Cited Publications

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Tpl2 Kinase Inhibitor 1

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Publications Citing Use of MedChemExpress (MCE) Tpl2 Kinase Inhibitor 1

All MAP3K Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tpl2 Kinase Inhibitor 1 Related Classifications

Cat. No.: HY-12358