| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
HFY-4A targets histone deacetylases (HDACs), a family of enzymes that remove acetyl groups from histone proteins and other substrates, thereby regulating gene expression through epigenetic modifications. By inhibiting HDAC activity, HFY-4A promotes the accumulation of acetylated histones, leading to relaxation of chromatin structure and transcriptional activation of tumor suppressor genes, cell cycle regulators, and pro-apoptotic factors. This mechanism underlies its antitumor activity against breast cancer cells.
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| ln Vitro |
In vitro, HFY-4A effectively inhibits breast cancer cell proliferation, migration, and invasion. The compound induces cell apoptosis (programmed cell death) in cancer cells through activation of intrinsic and/or extrinsic apoptotic pathways. Additionally, HFY-4A induces immunogenic cell death (ICD), a form of cell death that triggers an adaptive immune response against tumor antigens, potentially enhancing antitumor immunity. The compound is soluble in DMSO at 125 mg/mL (374.95 mM).
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| ln Vivo |
In vivo, HFY-4A demonstrates significant antitumor efficacy in a mouse model of breast cancer xenograft. In this model, human breast cancer cells are implanted subcutaneously into immunodeficient mice, and treatment with HFY-4A leads to suppression of tumor growth. The compound's ability to inhibit tumor growth in vivo, combined with its capacity to induce immunogenic cell death, suggests that HFY-4A may have potential for combination therapy with immunotherapeutic agents.
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| Enzyme Assay |
For non-cellular in vitro enzyme/receptor binding assays, HFY-4A is evaluated for its HDAC inhibitory activity using purified HDAC enzymes. The compound is incubated with HDAC enzyme and a fluorogenic substrate (such as a peptide containing an acetylated lysine residue). Upon enzymatic deacetylation, the substrate becomes susceptible to cleavage by a developer, releasing a fluorophore that can be quantified. The inhibitory activity is measured as the percentage of enzyme activity remaining at various compound concentrations, allowing calculation of the IC₅₀ value for HDAC inhibition.
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| Cell Assay |
For in vitro cellular assays, HFY-4A is tested in breast cancer cell lines to assess its antiproliferative and pro-apoptotic effects. Cells are seeded in culture plates and treated with serial dilutions of the compound for specified durations. Cell viability is measured using MTT, CCK-8, or similar assays. Apoptosis is detected by Annexin V-FITC/PI double staining followed by flow cytometry analysis. Cell migration and invasion are assessed using transwell or scratch wound healing assays. Immunogenic cell death markers such as calreticulin exposure, ATP release, and HMGB1 secretion may also be measured.
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| Animal Protocol |
For in vivo animal studies, HFY-4A is evaluated in a breast cancer xenograft mouse model. Female immunodeficient mice are inoculated subcutaneously with human breast cancer cells. When tumors reach a certain volume, mice are randomized into treatment and control groups. HFY-4A is administered at appropriate doses via intraperitoneal injection or oral gavage. Tumor volumes are measured twice weekly using calipers, and tumor growth inhibition is calculated. Body weight and general health status are monitored throughout the study to assess tolerability.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HFY-4A are not extensively documented. As a small-molecule HDAC inhibitor with a molecular weight of 333.38, it is expected to have favorable oral bioavailability and tissue distribution. The compound is soluble in DMSO, allowing for formulation in various vehicles for in vivo administration. Powder can be stored at -20°C for up to 3 years, and stock solutions in solvent can be stored at -80°C for 6 months or at -20°C for 1 month. Further pharmacokinetic studies would be needed to fully characterize its ADME profile.
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| Toxicity/Toxicokinetics |
Toxicological data for HFY-4A are limited. As an HDAC inhibitor, it may have dose-dependent toxicities associated with epigenetic modulation, potentially affecting normal cell function and proliferation. However, the compound's ability to induce immunogenic cell death and its antitumor activity in breast cancer xenograft models suggest a favorable therapeutic window. Comprehensive toxicology studies including acute and repeat-dose toxicity, genotoxicity, and organ-specific toxicity assessments would be required for clinical development. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
HFY-4A is a novel HDAC inhibitor that demonstrates potent antitumor activity against breast cancer through inhibition of cell proliferation, migration, and invasion, as well as induction of apoptosis and immunogenic cell death. The compound suppresses tumor growth in breast cancer xenograft mouse models. Its mechanism involves epigenetic modulation through HDAC inhibition, leading to transcriptional activation of genes involved in tumor suppression and apoptosis. HFY-4A was reported in a study published in Toxicology and Applied Pharmacology (2023), which demonstrated that the HDAC inhibitor improves TUSC2 transcription to induce immunogenic cell death in breast cancer.
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| CAS # |
2094810-82-7
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| Appearance |
White to off-white solid powder
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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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