| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| 10mg | |||
| Other Sizes |
| Targets |
LIMK1 9.8 nM (IC50) LIMK2 13 nM (IC50)
LIMK1 (LIM kinase 1) and LIMK2 (LIM kinase 2). |
|---|---|
| ln Vitro |
TH470 (0.05–5 μM; 12 h) prevents neurite growth[1].
TH470 is a highly selective inhibitor of LIMK1 and LIMK2. In biochemical assays, it exhibits IC50 values of 9.8 nM for LIMK1 and 13 nM for LIMK2, demonstrating its potent and specific inhibitory activity against these kinases. The compound effectively modulates the actin cytoskeleton and related cellular processes by inhibiting LIM kinase activity. |
| ln Vivo |
Not available in the public domain. As a selective kinase inhibitor, TH470 would typically be evaluated in animal models of orphan diseases to assess its in vivo efficacy, pharmacokinetics, and pharmacodynamics. Such studies would likely measure tumor growth inhibition or functional recovery in disease-relevant models.
|
| Enzyme Assay |
The compound is tested in enzymatic assays using recombinant LIMK1 and LIMK2 proteins. Kinase activity is measured in the presence of varying concentrations of TH470 to determine the IC50 values. The assay typically involves quantifying the phosphorylation of a specific substrate peptide using radioactive or fluorescence-based detection methods.
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: N1E -115 cells transfected with siRNAs against FMR1 (siFMR1) or control siRNAs (siCtr) Tested Concentrations: 0.05, 0.5, or 5 μM Incubation Duration: 12 hrs (hours) Experimental Results: Inhibited neurite outgrowth in a dose-dependent manner. Cellular assays are performed to evaluate the inhibitory effect of TH470 on LIMK-mediated signaling in cell lines. Cells are treated with TH470, and the phosphorylation levels of downstream targets such as cofilin are measured by Western blot to confirm target engagement and pathway inhibition. |
| ADME/Pharmacokinetics |
Physicochemical properties: Molecular Weight = 605.73, Molecular Formula = C30H31N5O5S2. Storage: Powder -20degC for 3 years; In solvent -80degC for 1 year. Shipping: Blue ice or at ambient temperature.
|
| References | |
| Additional Infomation |
TH470 (CAS#: 2834739-51-2) is a research-grade compound supplied for preclinical studies. Its high selectivity for LIMK1/2 makes it a valuable tool for dissecting the specific roles of these kinases in cellular processes like actin dynamics, cell migration, and proliferation. It is not approved for clinical use and is intended for research purposes only, particularly in the context of orphan disease research.
|
| Molecular Formula |
C30H31N5O5S2
|
|---|---|
| Molecular Weight |
605.73
|
| Exact Mass |
605.176
|
| CAS # |
2834739-51-2
|
| PubChem CID |
162369728
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
42
|
| Complexity |
1000
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C1C=CC(=CC=1)C(=O)N(CCNC(C1=CN=C(S1)NC(=O)C(C)C)=O)CC1C=CC=CC=1)(=O)(=O)NC1C=CC=CC=1
|
| InChi Key |
YVPYJSSYGACUSE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C30H31N5O5S2/c1-21(2)27(36)33-30-32-19-26(41-30)28(37)31-17-18-35(20-22-9-5-3-6-10-22)29(38)23-13-15-25(16-14-23)42(39,40)34-24-11-7-4-8-12-24/h3-16,19,21,34H,17-18,20H2,1-2H3,(H,31,37)(H,32,33,36)
|
| Chemical Name |
N-[2-[benzyl-[4-(phenylsulfamoyl)benzoyl]amino]ethyl]-2-(2-methylpropanoylamino)-1,3-thiazole-5-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~165.1 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.13 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.13 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6509 mL | 8.2545 mL | 16.5090 mL | |
| 5 mM | 0.3302 mL | 1.6509 mL | 3.3018 mL | |
| 10 mM | 0.1651 mL | 0.8255 mL | 1.6509 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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