Art. -Nr.: HY-172199

THX6

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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 (K_i = 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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Reinheit: 99.97%
CAS. Nr.: 3076954-42-9
Formel: C₂₂H₁₈Cl₂N₄O₂
Molecular Weight:441.31

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

THX6 Chemical Structure

CAS. Nr.: 3076954-42-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

hClpP

1.18 μM (EC₅₀)

In Vitro

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 (K_i > 100 μM) and hD3R (K_i = 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.

Western Blot Analysis^[1]

Cell Line:

SU-DIPG-36 cells
Concentration:

1.18 μM
Incubation Time:

24 h
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).

Real Time qPCR^[1]

Cell Line:

SU-DIPG-36 cells
Concentration:

1.18 μM
Incubation Time:

24 h
Result:

Decreased mtDNA copy number.

Chemical Information

CAS. Nr. 3076954-42-9
Appearance Solid
Molecular Weight 441.31
Formel C₂₂H₁₈Cl₂N₄O₂
Color White to light yellow
SMILES

N#CC1=CC=CC(CN2CCC3=C(C(N(C(N3)=O)CC4=CC=C(C(Cl)=C4)Cl)=O)C2)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2660 mL

11.3299 mL

22.6598 mL

5 mM

0.4532 mL

2.2660 mL

4.5320 mL

10 mM

0.2266 mL

1.1330 mL

2.2660 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Miciaccia M, et al., ONC201-Derived Tetrahydropyridopyrimidindiones as Powerful ClpP Protease Activators to Tackle Diffuse Midline Glioma. J Med Chem. 2025 Mar 13;68(5):5190-5210. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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THX6

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

THX6

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

THX6 Related Classifications

HY-172199 Related Classifications