LX7101
Based on 3 publication(s) in Google Scholar
LX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.54%
- No. CAS: 1192189-69-7
- Fòrmula: C23H29N7O3
- Peso molecular:451.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) LX7101
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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WB
Actividad biológica
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LIMK2 1.6 nM (IC50) |
LIMK1 24 nM (IC50) |
ROCK2 10 nM (IC50) |
PKA <1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A7R5 | EC50 |
2300 nM
Compound: LX-7101
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Inhibition of ROCK in rat A7r5 cells assessed as reduction in MLC Thr18/Ser19 phosphorylation by direct-ELISA method
Inhibition of ROCK in rat A7r5 cells assessed as reduction in MLC Thr18/Ser19 phosphorylation by direct-ELISA method
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[PMID: 26233434] |
| HeLa | EC50 |
55 μM
Compound: LX7101
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Cytotoxicity against human HeLa cells assessed as induction of cell death measured after 48 hrs by celltiter glo luminescent cell viability assay
Cytotoxicity against human HeLa cells assessed as induction of cell death measured after 48 hrs by celltiter glo luminescent cell viability assay
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[PMID: 38669909] |
| HeLa | EC50 |
8.7 nM
Compound: LX-7101
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Inhibition of LIMK in human HeLa cells assessed as reduction in cofilin Ser3 phosphorylation by sandwich immunoassay
Inhibition of LIMK in human HeLa cells assessed as reduction in cofilin Ser3 phosphorylation by sandwich immunoassay
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[PMID: 26233434] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1192189-69-7
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Appearance Solid
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Peso molecular 451.52
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Fòrmula C23H29N7O3
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Color White to off-white
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SMILES
NCC1(C(NC2=CC(OC(N(C)C)=O)=CC=C2)=O)CCN(C3=C4C(NC=C4C)=NC=N3)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Oncogene
LIMK2 promotes melanoma tumor growth and metastasis through G3BP1-ESM1 pathway-mediated apoptosis inhibition. [Abstract]2023 May;42(18):1478-1491. PMID: 36922679
LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 May;42(18):1478-1491. [Abstract]
Both LX7101 (5 μM) and TH-257 (5 μM) inhibits the colony-forming ability of melanoma cells (A375-MA2, MeWo, and SK-MEL-147 cells) in soft-agar.
LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 May;42(18):1478-1491. [Abstract]
Both LX7101 (5 μM; 24 h) and TH-257 (5 μM; 24 h) reduces the phosphorylation of G3BP1 in A375-MA2 and SK-MEL-147 cells.
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Sci Rep
Loss of the fragile X mental retardation protein causes aberrant differentiation in human neural progenitor cells. [Abstract]2018 Aug 2;8(1):11585. PMID: 30072797
LX7101 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Aug 2;8(1):11585. [Abstract]
Western blot analysis of GFAP protein levels in LX7101 and DMSO-treated iNPC-KO lines. GAPDH is used as a loading control.
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Solvente y solubilidad
DMSO : 150 mg/mL (332.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (16.61 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (16.61 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Boland S, et al. Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorganic & Medicinal Chemistry Letters (2015), 25(18), 4005-4010. [Content Brief]
[2]. Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL | 55.3685 mL |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | 11.0737 mL | |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL | 5.5369 mL | |
| 15 mM | 0.1476 mL | 0.7382 mL | 1.4765 mL | 3.6912 mL | |
| 20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7684 mL | |
| 25 mM | 0.0886 mL | 0.4429 mL | 0.8859 mL | 2.2147 mL | |
| 30 mM | 0.0738 mL | 0.3691 mL | 0.7382 mL | 1.8456 mL | |
| 40 mM | 0.0554 mL | 0.2768 mL | 0.5537 mL | 1.3842 mL | |
| 50 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1074 mL | |
| 60 mM | 0.0369 mL | 0.1846 mL | 0.3691 mL | 0.9228 mL | |
| 80 mM | 0.0277 mL | 0.1384 mL | 0.2768 mL | 0.6921 mL | |
| 100 mM | 0.0221 mL | 0.1107 mL | 0.2215 mL | 0.5537 mL |
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