country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-125444

Copy Link Print Information

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1622059-04-4
Formel: C₂₂H₂₂N₂O₃S
Molecular Weight:394.49

Speicherung:

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

TH251 Chemical Structure

CAS. Nr.: 1622059-04-4

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

human LIMK1

52 nM (IC₅₀)

LIMK2

Alle LIM Kinase (LIMK) Isoform-spezifische Produkte anzeigen :

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]

In Vitro

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.

In Vivo

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.

Chemical Information

CAS. Nr. 1622059-04-4
Molecular Weight 394.49
Formel C₂₂H₂₂N₂O₃S
SMILES

O=C(C1=CC=C(C=C1)S(=O)(=O)NC=2C=CC=CC2)N(CC=3C=CC=CC3)CC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

TH251

Alle LIM Kinase (LIMK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

TH251 Related Classifications

HY-125444 Related Classifications