2. Cell Cycle/DNA Damage
  3. ClpP
  4. THX6

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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THX6

THX6 Chemical Structure

CAS No. : 3076954-42-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

THX6 Related Antibodies

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Description

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[1].

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 (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.

THX6 Related Antibodies

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.
Molecular Weight

441.31

Formula

C22H18Cl2N4O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2660 mL 11.3299 mL 22.6598 mL
5 mM 0.4532 mL 2.2660 mL 4.5320 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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:

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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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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THX6 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

THX63076954-42-9THX 6THX-6ClpPCaseinolytic protease PActivatorhD3RHEK293 cellsfatty acidsDIPG cellsdiffuse intrinsic pontine gliomaInhibitorinhibitorinhibit

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