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製品番号: HY-125444

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TH251

TH251 is a LIMK1 and LIMK2 inhibitor with IC₅₀s of 52 nM and 47 nM against LIMK1 and LIMK2, respectively. TH251 binds to inactive αC-out and DFG-out LIMK1 conformations, inhibits unphosphorylated LIMK1 and LIMK2 enzymatic activity, and exhibits unchanged potency despite PAK-mediated phosphorylation of either kinase. TH251 can be used for the research of cancers, glaucoma, and CNS diseases.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 1622059-04-4
分子式: C₂₂H₂₂N₂O₃S
分子量:394.49

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

TH251 構造式

CAS 番号: 1622059-04-4

容量

価格（税別）

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数量

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Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

human LIMK1

52 nM (IC₅₀)

LIMK2

LIM Kinase (LIMK) アイソフォーム固有の製品をすべて表示 :

LIMK1
LIMK2

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.003 μM Compound: 31	Inhibition of human full-length LIMK2 expressed in Sf9 cells assessed as incorporation of [33P] from ATP into biotinylated-cofilin substrate in presence of 300 uM ATP Inhibition of human full-length LIMK2 expressed in Sf9 cells assessed as incorporation of [33P] from ATP into biotinylated-cofilin substrate in presence of 300 uM ATP	[PMID: 25589930]

体外実験

TH251 (Compound 22) (45-180 min) potently inhibits LIMK2 (pIC₅₀ = 7.90) and PAK-phosphorylated LIMK2 (pIC₅₀ = 8.19) with greater potency than against LIMK1 and PAK-phosphorylated LIMK1 in purified enzyme assays^[1].
TH251 potently inhibits human LIMK1 kinase activity (IC₅₀ = 52 nM) and human LIMK2 kinase activity (IC₅₀ = 47 nM) in a mass spectrometry-based kinase assay using CFL1 as the substrate^[2].

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

体内実験

TH251 (1-50 μM) (Compound 22) rescues hyperactive crawling and elevated neuromuscular junction bouton number in dFMR1 mutant Drosophila larvae, normalizing these Fragile X syndrome-related phenotypes^[2].

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

化学情報

CAS 番号 1622059-04-4
分子量 394.49
分子式 C₂₂H₂₂N₂O₃S
SMILES

O=C(C1=CC=C(C=C1)S(=O)(=O)NC=2C=CC=CC2)N(CC=3C=CC=CC3)CC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Collins R, et al. Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. J Med Chem. 2022 Oct 27;65(20):13705-13713. [Content Brief]

[2]. Mathea, S; et al. LIM Domain Kinase 1 (LIMK1), Human Kinase Domain; A Target Enabling Package. University of Oxford, 2017 Jun 2.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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TH251

LIM Kinase (LIMK) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

TH251 関連分類

HY-125444 関連分類