2. Epigenetics Apoptosis
  3. Histone Acetyltransferase Apoptosis
  4. TH1834

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

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TH1834 Chemical Structure

TH1834 Chemical Structure

CAS No. : 2108830-08-4

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10 mg USD 290 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of TH1834:

TH1834 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TH1834

View All Histone Acetyltransferase Isoform Specific Products:

View All Isoforms
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

TIP60

 

In Vitro

TH1834 (0-500 μM; 1 hour; MCF7 cells) treatment significantly reduces the viability of MCF7 cells[1].
TH1834 (0-500 μM; 1 hour; MCF7 cells) treatment significantly increases cytotoxicity in MCF7 cells[1].
TH1834 (500 μM; 1 hour; MCF7 cells) treatment induces caspase 3 activation in MCF7 cells[1].
TH1834 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.

TH1834 Related Antibodies

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

568.71

Formula

C33H40N6O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)CN1N=C(C2=CC=C(CN(CCC3=CC=CC=C3)CCCCOC4=CC=C(CN5CCCC5)C=C4)C=C2)N=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (17.58 mM; ultrasonic and warming and heat to 60°C; 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 1.7584 mL 8.7918 mL 17.5837 mL
5 mM 0.3517 mL 1.7584 mL 3.5167 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)

Mass
=
Concentration
×
Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 1 mg/mL (1.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (1.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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

Purity: 99.60%

COA (245 KB) HNMR (142 KB) RP-HPLC (126 KB)

Handling Instructions (2659 KB)
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 1.7584 mL 8.7918 mL 17.5837 mL 43.9591 mL
5 mM 0.3517 mL 1.7584 mL 3.5167 mL 8.7918 mL
10 mM 0.1758 mL 0.8792 mL 1.7584 mL 4.3959 mL
15 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9306 mL
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TH1834 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:

TH18342108830-08-4TH 1834TH-1834Histone AcetyltransferaseApoptosisHATsHATTip60DNAdamageapoptosisbreastcancerPNTcaspase-3cytotoxicityInhibitorinhibitorinhibit

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