| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Histone Acetyltransferase Inhibitor II specifically targets p300 histone acetyltransferase (HAT), also referred to as p300/CBP-associated factor. It acts as an antagonist of p300, inhibiting its enzymatic activity with an IC50 of 5 µM. p300 is a critical transcriptional coactivator that acetylates histone and non-histone proteins, regulating diverse cellular processes including proliferation, differentiation, and apoptosis.
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| ln Vitro |
In HeLa-H2B-EYFP cells, Histone Acetyltransferase Inhibitor II (20–40 μM) lowers H3 acetylation levels [1].
In vitro, Histone Acetyltransferase Inhibitor II demonstrates potent anti-acetylase activity in mammalian cells. In HeLa-H2B-EYFP cells, treatment with 20–40 µM of the compound significantly lowers histone H3 acetylation levels. The compound effectively penetrates cells and inhibits p300-mediated acetylation, providing a valuable tool for studying the functional consequences of histone acetylation in various cellular contexts. |
| ln Vivo |
In vivo activity data for Histone Acetyltransferase Inhibitor II are limited, as the compound is primarily utilized as a research tool for in vitro epigenetic studies. It has been suggested to have potential therapeutic applications in cancer, inflammation, and neurodegenerative diseases based on its mechanism of action, but systematic in vivo efficacy studies have not been extensively reported. Further investigations are needed to characterize its pharmacokinetic and pharmacodynamic profiles in animal models.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for Histone Acetyltransferase Inhibitor II typically involves measuring its ability to inhibit p300 HAT activity using purified enzyme preparations. The assay is conducted in cell-free systems with histone substrates and acetyl-CoA, and the inhibitory activity is quantified by IC50 determination. For this compound, the IC50 against p300 HAT is 5 µM. Reaction products are detected using radiometric, fluorometric, or ELISA-based methods to assess the extent of histone acetylation.
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| Cell Assay |
In vitro cellular assays are performed using mammalian cell lines such as HeLa-H2B-EYFP cells. Cells are treated with Histone Acetyltransferase Inhibitor II at concentrations ranging from 20–40 µM for specified durations. Following treatment, histone acetylation levels are assessed by Western blotting using acetylation-specific antibodies, typically targeting histone H3 or H4. The compound's cell permeability and anti-acetylase activity are evaluated by comparing acetylation levels between treated and untreated control cells.
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| Animal Protocol |
In vivo animal experimental protocols for Histone Acetyltransferase Inhibitor II are not well established in the published literature, as this compound is predominantly used for in vitro research applications. For in vivo administration, the compound can be formulated in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline, with a solubility of at least 2.5 mg/mL (5.39 mM). Oral administration in CMC-Na suspension at concentrations up to 5 mg/mL has also been described.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Histone Acetyltransferase Inhibitor II have not been systematically characterized in the literature. Based on its physicochemical properties (molecular weight 464.15, LogP 5.842), the compound is highly lipophilic, which may influence its absorption, distribution, metabolism, and excretion profile. It is soluble in DMSO (≥30 mg/mL, ~64.63 mM) but has limited aqueous solubility. Further PK studies are needed to determine its half-life, bioavailability, and tissue distribution.
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| Toxicity/Toxicokinetics |
Toxicological data for Histone Acetyltransferase Inhibitor II are not extensively reported in the available literature. As a research-use compound, its safety profile has not been formally evaluated in preclinical toxicology studies. The compound is intended for in vitro research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment.
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| References | |
| Additional Infomation |
Histone Acetyltransferase Inhibitor II (compound 2c) is a research-grade chemical supplied with purity ≥98%. Its molecular formula is C20H16Br2O3 and molecular weight is 464.15. The compound is a light yellow to yellow solid powder and should be stored at -20°C for long-term stability (up to 3 years). It is classified as an epigenetic research tool and is not intended for diagnostic or therapeutic applications.
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| Molecular Formula |
C20H16BR2O3
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|---|---|
| Molecular Weight |
464.1472
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| Exact Mass |
461.947
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| CAS # |
932749-62-7
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| PubChem CID |
16203606
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.842
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
511
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C/C(=C\C2=CC(=C(C=C2)O)Br)/C(=O)/C(=C/C3=CC(=C(C=C3)O)Br)/C1
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| InChi Key |
YOLKEKNTCBWPSD-VOMDNODZSA-N
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| InChi Code |
InChI=1S/C20H16Br2O3/c21-16-10-12(4-6-18(16)23)8-14-2-1-3-15(20(14)25)9-13-5-7-19(24)17(22)11-13/h4-11,23-24H,1-3H2/b14-8+,15-9+
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| Chemical Name |
(2E,6E)-2,6-bis[(3-bromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one
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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 : ≥ 30 mg/mL (~64.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1545 mL | 10.7724 mL | 21.5448 mL | |
| 5 mM | 0.4309 mL | 2.1545 mL | 4.3090 mL | |
| 10 mM | 0.2154 mL | 1.0772 mL | 2.1545 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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