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Cat. No.: 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.

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CAS No.: 1622059-04-4
화학식: C₂₂H₂₂N₂O₃S
분자량:394.49

보관:

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

TH251 Chemical Structure

CAS No.: 1622059-04-4

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

human LIMK1

52 nM (IC₅₀)

LIMK2

All LIM Kinase (LIMK) Isoforms :

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 No. 1622059-04-4
분자량 394.49
화학식 C₂₂H₂₂N₂O₃S
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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TH251

All LIM Kinase (LIMK) Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

TH251 Related Classifications

HY-125444 Related Classifications