THX6
Based on 1 Customer Validation
THX6 is an hClpP activator with an EC50 of 1.18 μM. THX6 improves off-target profile with no affinity for hD2R and only weak affinity for hD3R (Ki = 51.1 µM) in HEK293 cells. THX6 shows good cytotoxicity in ONC201-resistant cells with an IC50 of 0.13 μM. THX6 changes the levels of fatty acids (PUFAs, MUFAs, and SFAs) in DIPG cells. THX6 decreases the level of proteins involved in oxidative phosphorylation, biogenesis, and mitophagy proteins, thereby resulting in a global collapse of mitochondrial integrity and function. THX6 can be used for diffuse intrinsic pontine glioma research.
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- Pureza: 99.97%
- No. CAS: 3076954-42-9
- Fòrmula: C22H18Cl2N4O2
- Peso molecular:441.31
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
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Actividad biológica
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hClpP 1.18 μM (EC50) |
THX6 (compound 36) stabilizes hClpP in Caco-2 cells, demonstrating potent and effective target engagement and stabilization[1].
THX6 increases the proteolytic activity of hClpP with an IC50 value of 1.18 μM[1].
THX6 shows superior selectivity by demonstrating negligible binding to hD2R (Ki > 100 μM) and hD3R (Ki = 26.7μM) in competitive binding assays using HEK293 cells[1].
THX6 (0.19-200 μM, 72 h) exhibits cytotoxicity in the micromolar range in SU-DIPG-36 (mutant H3.1K27M) SU-DIPG-50 (mutant H3.3K27M), HSJD-007 (mutant H3.3K27M) , SF8628 (mutant H3.3K27M) and SU-DIPG-VI (mutant H3.3K27M) with IC50 values of 47.7, > 100 0.46, 468 and 10.89 μM, respectively[1].
THX6 (1.18 μM, 24 h) acts as an hClpXP agonist by promoting hClpX dissociation and degradation, suppresses mitochondrial oxidative phosphorylation, biogenesis, and mitophagy in the SU DIPG-36CellLine in SU-DIPG-36 cells[1].
THX6 (24 h) selectively reduces the levels of highly unsaturated fatty acids (PUFAs/MUFAs) in SH-SY5Y and SU-DIPG-50 cell lines, but not in SU-DIPG-36 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DIPG-36 cells
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Concentration:1.18 μM
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Incubation Time:24 h
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Result:Strongly decreased the level of the hClpX chaperone subunit and did not appear to affect the amount of hClpP Observed a strong decline of SDHA and ATP5A (nuclear-encoded subunits of complexes II andV).
Observed a strong decline of COI (mitochondrial (mt)DNA encoded subunit of complex IV).
Significantly diminished the level of NRF1 and, more markedly TFAM (those protein involve in mitochondrial biogenesis).
Observed a decline of TOMM20 protein, which indicating a decrease mitochondrial mass.
Observed a reduction of the Parkin (an mitophagy markers).
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Cell Line:SU-DIPG-36 cells
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Concentration:1.18 μM
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Incubation Time:24 h
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Result:Decreased mtDNA copy number.
Chemical Information
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No. CAS 3076954-42-9
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Appearance Solid
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Peso molecular 441.31
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Fòrmula C22H18Cl2N4O2
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Color White to light yellow
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SMILES
N#CC1=CC=CC(CN2CCC3=C(C(N(C(N3)=O)CC4=CC=C(C(Cl)=C4)Cl)=O)C2)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (226.60 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)
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: ≥ 2.5 mg/mL (5.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (273 KB)
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SDS (251 KB)
- English - EN (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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2660 mL | 11.3299 mL | 22.6598 mL | 56.6495 mL |
| 5 mM | 0.4532 mL | 2.2660 mL | 4.5320 mL | 11.3299 mL | |
| 10 mM | 0.2266 mL | 1.1330 mL | 2.2660 mL | 5.6650 mL | |
| 15 mM | 0.1511 mL | 0.7553 mL | 1.5107 mL | 3.7766 mL | |
| 20 mM | 0.1133 mL | 0.5665 mL | 1.1330 mL | 2.8325 mL | |
| 25 mM | 0.0906 mL | 0.4532 mL | 0.9064 mL | 2.2660 mL | |
| 30 mM | 0.0755 mL | 0.3777 mL | 0.7553 mL | 1.8883 mL | |
| 40 mM | 0.0566 mL | 0.2832 mL | 0.5665 mL | 1.4162 mL | |
| 50 mM | 0.0453 mL | 0.2266 mL | 0.4532 mL | 1.1330 mL | |
| 60 mM | 0.0378 mL | 0.1888 mL | 0.3777 mL | 0.9442 mL | |
| 80 mM | 0.0283 mL | 0.1416 mL | 0.2832 mL | 0.7081 mL | |
| 100 mM | 0.0227 mL | 0.1133 mL | 0.2266 mL | 0.5665 mL |
THX6 Related Classifications
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