1. Epigenetics Apoptosis
  2. Histone Acetyltransferase Apoptosis
  3. TH1834 dihydrochloride

TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.

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TH1834 dihydrochloride Chemical Structure

TH1834 dihydrochloride Chemical Structure

CAS No. : 2108830-09-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of TH1834 dihydrochloride:

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  • Purity & Documentation

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Description

TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity[1].

In Vitro

TH1834 dihydrochloride (0-500 μM; 1 hour; MCF7 cells) treatment significantly reduces the viability of MCF7 cells[1].
TH1834 dihydrochloride (0-500 μM; 1 hour; MCF7 cells) treatment highly significant increase in cytotoxicity[1].
TH1834 dihydrochloride (500 μM; 1 hour; MCF7 cells) treatment induces caspase 3 activation in MCF7 cells[1].
TH1834 dihydrochloride significantly inhibits Tip60 activity in vitro and treating cells with TH1834 results in apoptosis and increased unrepaired DNA damage in breast cancer[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF7 cells
Concentration: 0 μM, 0.5 μM, 5 μM, 50 μM and 500 μM
Incubation Time: 1 hour
Result: Significantly reduced the viability of MCF7 cells.

Cell Cytotoxicity Assay[1]

Cell Line: MCF7 cells
Concentration: 0 μM, 0.5 μM, 5 μM, 50 μM and 500 μM
Incubation Time: 1 hour
Result: Highly significant increase in cytotoxicity at all concentrations used.

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 500 μM
Incubation Time: 1 hour
Result: Marked caspase 3 activation was observed in MCF7 cells in an independent assay.
Molecular Weight

641.63

Formula

C33H42Cl2N6O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CN1N=C(C2=CC=C(CN(CCC3=CC=CC=C3)CCCCOC4=CC=C(CN5CCCC5)C=C4)C=C2)N=N1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (155.85 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (155.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5585 mL 7.7927 mL 15.5853 mL
5 mM 0.3117 mL 1.5585 mL 3.1171 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 2.08 mg/mL (3.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 25 mg/mL (38.96 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.68%

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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 1.5585 mL 7.7927 mL 15.5853 mL 38.9633 mL
5 mM 0.3117 mL 1.5585 mL 3.1171 mL 7.7927 mL
10 mM 0.1559 mL 0.7793 mL 1.5585 mL 3.8963 mL
15 mM 0.1039 mL 0.5195 mL 1.0390 mL 2.5976 mL
20 mM 0.0779 mL 0.3896 mL 0.7793 mL 1.9482 mL
25 mM 0.0623 mL 0.3117 mL 0.6234 mL 1.5585 mL
30 mM 0.0520 mL 0.2598 mL 0.5195 mL 1.2988 mL
40 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9741 mL
50 mM 0.0312 mL 0.1559 mL 0.3117 mL 0.7793 mL
60 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6494 mL
80 mM 0.0195 mL 0.0974 mL 0.1948 mL 0.4870 mL
100 mM 0.0156 mL 0.0779 mL 0.1559 mL 0.3896 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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TH1834 dihydrochloride 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.

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