LC-04-045
Based on 1 Customer Validation
LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.56%
- Fòrmula: C32H28ClN5O3
- Peso molecular:566.05
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
NEK7 7 nM (DC50) |
IL-1β |
IL-18 |
In Vitro
LC-04-045 (0.007 μM; 6 h) potently degrades NEK7 in MOLT-4 cells with a DC50 of 7 nM and a Dmax of 90%[1].
LC-04-045 (37 nM-10 μM; 0-24 h) induces time-dependent NEK7 degradation in MOLT-4 cells[1].
LC-04-045 promotes formation of a CRBN:MGD:NEK7 ternary complex in HEK293T cells with an EC50 of 33 nM[1].
LC-04-045 (6 h) selectively degrades wildtype NEK7, but not NEK7 variants with G57N, R35A, or R50A mutations, in MOLT-4 cells after 6 h of treatment, confirming dependence on the G57-containing degron motif and adjacent R35/R50 residues for activity[1].
LC-04-045 (37 nM-10 μM; 24 h) potently degrades NEK7 in PBMCs with a DC50 of 2.9 nM and a Dmax of 90% after 24 h of treatment[1].
LC-04-045 (1.5 nM-10 μM; 16 h) potently degrades NEK7 in LPS (HY-D1056)-stimulated hMDMs with a DC50 of 40 nM and a Dmax of 88%[1].
LC-04-045 (0.01 nM-10000 nM) effectively inhibits LPS-stimulated secretion of IL-1β (IC50 = 33.03 nM) and IL-18 (IC50 = 32.99 nM) in hMDMs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4
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Concentration:37, 111, 333 nM, 1, 10 μM
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Incubation Time:6 h
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Result:Induced time-dependent NEK7 degradation.
Did not affect protein levels of NEK1, NEK2, NEK4, NEK10, or NEK11.
Chemical Information
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Appearance Solid
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Peso molecular 566.05
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Fòrmula C32H28ClN5O3
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Color White to off-white
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SMILES
O=C([C@@H](N(CC1=C2C=CC(C3=CN=C4CN(CC5=CC=CC=C5C6=CC=CC=C6Cl)CCN43)=C1)C2=O)CC7)NC7=O
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (176.66 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 5 mg/mL (8.83 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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 (275 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7666 mL | 8.8331 mL | 17.6663 mL | 44.1657 mL |
| 5 mM | 0.3533 mL | 1.7666 mL | 3.5333 mL | 8.8331 mL | |
| 10 mM | 0.1767 mL | 0.8833 mL | 1.7666 mL | 4.4166 mL | |
| 15 mM | 0.1178 mL | 0.5889 mL | 1.1778 mL | 2.9444 mL | |
| 20 mM | 0.0883 mL | 0.4417 mL | 0.8833 mL | 2.2083 mL | |
| 25 mM | 0.0707 mL | 0.3533 mL | 0.7067 mL | 1.7666 mL | |
| 30 mM | 0.0589 mL | 0.2944 mL | 0.5889 mL | 1.4722 mL | |
| 40 mM | 0.0442 mL | 0.2208 mL | 0.4417 mL | 1.1041 mL | |
| 50 mM | 0.0353 mL | 0.1767 mL | 0.3533 mL | 0.8833 mL | |
| 60 mM | 0.0294 mL | 0.1472 mL | 0.2944 mL | 0.7361 mL | |
| 80 mM | 0.0221 mL | 0.1104 mL | 0.2208 mL | 0.5521 mL | |
| 100 mM | 0.0177 mL | 0.0883 mL | 0.1767 mL | 0.4417 mL |
LC-04-045 Related Classifications
HY-172162 Related Classifications
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