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.
For research use only. We do not sell to patients.
- CAS No.: 1622059-04-4
- Formula: C22H22N2O3S
- Molecular Weight:394.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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human LIMK1 52 nM (IC50) |
LIMK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.003 μM
Compound: 31
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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
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[PMID: 25589930] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1622059-04-4
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Molecular Weight 394.49
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Formula C22H22N2O3S
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SMILES
O=C(C1=CC=C(C=C1)S(=O)(=O)NC=2C=CC=CC2)N(CC=3C=CC=CC3)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TH251 Related Classifications
HY-125444 Related Classifications
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