2. MAPK/ERK Pathway
  3. MAP3K p38 MAPK MAPKAPK2 (MK2)
  4. Tpl2 Kinase Inhibitor 1

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.

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Tpl2 Kinase Inhibitor 1

Tpl2 Kinase Inhibitor 1 Chemische Struktur

CAS. Nr. : 871307-18-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Tpl2 Kinase Inhibitor 1:

Tpl2 Kinase Inhibitor 1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tpl2 Kinase Inhibitor 1

Alle MAP3K Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
MAP3K7/TAK1 MAP3K8/COT/Tpl2 MAP3K6/ASK2 MAP3K5/ASK1 MAP3K12/DLK/Pref-1 NIK/MAP3K14

Alle p38 MAPK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Beschreibung

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[1][2].

IC50 & Target[1]

MAP3K8/COT/Tpl2

 

p38

180 μM (IC50)

MK2

110 μM (IC50)

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.

Tpl2 Kinase Inhibitor 1 Related Antibodies
Molekulargewicht

404.83

Formel

C21H14ClFN6
CAS. Nr.
Appearance

Solid

Color

Yellow to green

SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4702 mL 12.3509 mL 24.7017 mL
5 mM 0.4940 mL 2.4702 mL 4.9403 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 99.42%

SDS (392 KB)

COA (249 KB) HNMR (119 KB) RP-HPLC (233 KB) MS (202 KB)

Handling Instructions (2659 KB)
Verweise

Complete Stock Solution Preparation Table

* 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.

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
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Tpl2 Kinase Inhibitor 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tpl2 Kinase Inhibitor 1871307-18-5MAP3Kp38 MAPKMAPKAPK2 (MK2)MAP kinase kinase kinase, MEKK, MAPKKKMitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2COTkinaseinflammatorycancerInhibitorinhibitorinhibit

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