| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
TH1834 targets Tip60 (KAT5), a histone acetyltransferase. It acts as a specific inhibitor of Tip60 HAT activity. TH1834 does not affect the activity of the related histone acetyltransferase MOF.
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|---|---|
| ln Vitro |
The viability of MCF7 cells is considerably reduced by TH1834 (0-500 μM; 1 hour) [1]. MCF7 cells treated with TH1834 (0-500 μM; 1 hour) exhibit a considerable increase in cytotoxicity [1]. MCF7 cells are exposed to 500 μM of TH1834 for one hour, which causes caspase 3 activation [1]. In vitro, TH1834 dramatically reduces Tip60 activity. In breast cancer, TH1834 treatment increases unrepaired DNA damage and induces death in cells [1].
In vitro, TH1834 is a specific Tip60 (KAT5) HAT inhibitor. It induces apoptosis and increases DNA damage in breast cancer cells. The compound has anti-cancer effects. Specific IC50 values are not provided in the available sources. |
| ln Vivo |
In vivo activity data for TH1834 are not extensively detailed in the available sources. The compound is a research tool for studying Tip60 function in breast cancer. Specific in vivo efficacy data in animal models have not been reported.
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| Enzyme Assay |
The in vitro enzyme assay for TH1834 involves measuring the inhibition of Tip60 HAT activity. Recombinant Tip60 is incubated with a histone substrate and acetyl-CoA in the presence of varying compound concentrations. The IC50 is determined by quantifying the reduction in histone acetylation using radioactive or fluorescence-based assays.
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: MCF7 cells Tested Concentrations: 0μM, 0.5μM, 5μM, 50μM and 500μM Incubation Duration: 1 hour Experimental Results: The viability of MCF7 cells was Dramatically diminished. Cytotoxicity assay[1] Cell Types: MCF7 Cell Tested Concentrations: 0 μM, 0.5 μM, 5 μM, 50 μM and 500 μM Incubation Duration: 1 hour Experimental Results: Cytotoxicity increased Dramatically at all concentrations used. Western Blot Analysis[1] Cell Types: MCF7 Cells Tested Concentrations: 500 μM Incubation Duration: 1 hour Experimental Results: In an independent assay, significant caspase 3 activation was observed in MCF7 cells. Cellular assays are performed using breast cancer cell lines. Cells are treated with TH1834 at varying concentrations. Apoptosis is assessed by measuring caspase activity or Annexin V staining. DNA damage is assessed by measuring γH2AX foci formation. |
| Animal Protocol |
In vivo animal studies for TH1834 are not detailed in the available sources. The compound is a research tool for studying Tip60 function in breast cancer. Specific animal models, dosing regimens, and efficacy data have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TH1834 are not available in the provided sources. The compound has a molecular weight of 568.71 g/mol. Powder formulations should be stored at -20°C. Specific PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for TH1834 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. Specific toxicological profiles have not been characterized.
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| References | |
| Additional Infomation |
TH1834 is a research compound for studying Tip60 function in cancer. It is a specific Tip60 (KAT5) HAT inhibitor that induces apoptosis and increases DNA damage in breast cancer cells. The compound is available from commercial suppliers for research use only.
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| Molecular Formula |
C33H40N6O3
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|---|---|
| Molecular Weight |
568.7091
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| Exact Mass |
568.316
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| CAS # |
2108830-08-4
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| Related CAS # |
TH1834 dihydrochloride;2108830-09-5
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| PubChem CID |
91826512
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| Appearance |
White to light yellow solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
42
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| Complexity |
761
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])C1C([H])=C([H])C(C2N=NN(C([H])([H])C(=O)O[H])N=2)=C([H])C=1[H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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| InChi Key |
XERATECPNBWJFP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H40N6O3/c40-32(41)26-39-35-33(34-36-39)30-14-10-28(11-15-30)25-38(22-18-27-8-2-1-3-9-27)21-6-7-23-42-31-16-12-29(13-17-31)24-37-19-4-5-20-37/h1-3,8-17H,4-7,18-26H2,(H,40,41)
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| Chemical Name |
2-[5-[4-[[2-phenylethyl-[4-[4-(pyrrolidin-1-ylmethyl)phenoxy]butyl]amino]methyl]phenyl]tetrazol-2-yl]acetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~17.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1758 mL | 0.8792 mL | 1.7584 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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