Tpl2 Kinase Inhibitor 1

Name: Tpl2 Kinase Inhibitor 1
Brand: MedChemExpress
SKU: HY-12358
Rating: 4.5 (1 reviews)

製品番号: HY-12358 純度: 99.42%: Data Sheet SDS COA 取扱説明書
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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 構造式

CAS 番号 : 871307-18-5

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 242	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 242	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$80	在庫あり	Estimated Time of Arrival: December 31
5 mg	$220	在庫あり	Estimated Time of Arrival: December 31
10 mg	$350	在庫あり	Estimated Time of Arrival: December 31
25 mg	$660	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1100	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1760	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Tpl2 Kinase Inhibitor 1:

Tpl2 Kinase Inhibitor 1 hydrochloride お問い合わせ

顧客検証

•Phytomedicine. 2024 Mar:125:155346.

MAP3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

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

p38 MAPK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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 3 Compound: 1b	Inhibition of EGFR kinase autophosphorylation in A431 cells Inhibition of EGFR kinase autophosphorylation in A431 cells	[PMID: 17664070]
A-431	IC₅₀	< 5 3 Compound: 1b	Inhibition of EGFR kinase autophosphorylation in A431 cells Inhibition of EGFR kinase autophosphorylation in A431 cells	[PMID: 17664070]
Monocyte	IC₅₀	1.1 3 Compound: 1b	Inhibition of LPS-induced TNFalpha production in human monocytes Inhibition of LPS-induced TNFalpha production in human monocytes	[PMID: 17664070]
Monocyte	IC₅₀	1.1 3 Compound: 1b	Inhibition of LPS-induced TNFalpha production in human monocytes Inhibition of LPS-induced TNFalpha production in human monocytes	[PMID: 17664070]

体外実験

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.

分子量

404.83

分子式

C₂₁H₁₄ClFN₆

CAS 番号

871307-18-5

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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
10 mM	0.2470 mL	1.2351 mL	2.4702 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 99.42%

Select Batch:

データシート (274 KB) SDS (392 KB)

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

取扱説明書 (2659 KB)

参考文献

[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]

Complete Stock Solution Preparation Table

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