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Purity: ≥98%
T56-LIMKi (also known as T5601640) is a potent and selective inhibitor of LIMK2 (LIM kinase 2) with an IC50 of 35.2 μM in a cell (Panc-1 cells) assay. T56-LIMKi exhibits little to no cross-reactivity with LIMK1 and inhibits LIMK2 with high specificity. T56-LIMKi inhibits the growth of multiple cancerous cell lines, such as those of glioma, schwannoma, and pancreatic cancer, by lowering the levels of phosphorylated cofilin (p-cofilin). T56-LIMKi lowered p-cofilin levels and tumor size in a panc-1 xenograft model in naked mice. LIM kinases are significant regulators of the cell cytoskeleton and are involved in the development, metastasis, and expression of cancer as well as disorders of the nervous system. T56-LIMKi may therefore be developed as a candidate medication for neuronal disorders and cancer therapy.
| Targets |
LIMK2
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
T56-LIMKi (also known as T5601640) is a powerful and focused inhibitor of LIMK2 (LIM kinase 2), exhibiting an IC50 of 35.2 μM in a cell assay using Panc-1 cells.
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| Cell Assay |
T56-LIMKi can cause Panc-1 tumor shrinkage and cofilin phosphorylation inhibition in vivo. Tumor volume in mice treated with T56-LIMKi (60 mg/kg) is significantly lower than in control mice[1].
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| Animal Protocol |
Mice: In a 0.5% carboxymethylcellulose solution, T56-LIMKi is dissolved. Panc-1 xenografts are injected into mice. Seven days later, treatment is initiated. Mice in the control group are given only the vehicle (0.5% CMC) in the gavage, while mice in the two experimental groups are given daily oral non-toxic doses of T56-LIMKi (30 or 60 mg/kg)[1].
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| References |
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| Molecular Formula |
C19H14F3N3O3
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|---|---|---|
| Molecular Weight |
389.33
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| Exact Mass |
389.098
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| Elemental Analysis |
C, 58.62; H, 3.62; F, 14.64; N, 10.79; O, 12.33
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| CAS # |
924473-59-6
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| Related CAS # |
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| PubChem CID |
9438169
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
403.4±45.0 °C at 760 mmHg
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| Flash Point |
197.8±28.7 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.618
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| LogP |
2.85
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
572
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC(C)=NO1)NC1C=C(C(NC2C=C(C(F)(F)F)C=CC=2)=O)C=CC=1
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| InChi Key |
XVOKFRPKSAWELK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H14F3N3O3/c1-11-8-16(28-25-11)18(27)24-14-6-2-4-12(9-14)17(26)23-15-7-3-5-13(10-15)19(20,21)22/h2-10H,1H3,(H,23,26)(H,24,27)
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| Chemical Name |
3-methyl-N-[3-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl]-1,2-oxazole-5-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO:≥ 40 mg/mL
Water: Ethanol: |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5685 mL | 12.8426 mL | 25.6852 mL | |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.1370 mL | |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 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.
T56-LIMKi inhibits LIMK2-mediated phosphorylation of cofilin. |
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ROCK inhibitor Y-27632 mask T56-LIMKi inhibition of cofilin phosphorylation. |
T56-LIMKi inhibits proliferation of various cancer cell lines in a cell-line specific manner. |
Levels of p-cofilin levels are reduced in a cell-specific manner by T56-LIMKi. |
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T-56-LIMKi inhibits proliferation of Panc-1 tumor cells in nude mice. |
T56-LIMKi reduces p-cofilin levels in Panc1- cell xenografts in a nude mouse model. |
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