| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
HC-Toxin targets histone deacetylases (HDACs), a family of enzymes that remove acetyl groups from histone proteins, thereby regulating gene expression. The compound inhibits HDACs in maize, Physarum, and chicken. By inhibiting HDACs, HC-Toxin alters chromatin structure and modulates the transcription of genes involved in cell cycle regulation, differentiation, and apoptosis. The compound has an IC50 of 30 nM for HDAC inhibition. This mechanism of action is shared with other HDAC inhibitors used in cancer research and therapy.
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| ln Vitro |
In a dose-dependent manner, HC-Toxin demonstrated strong antiproliferative activity and cell cycle arrest in the G2/M phase in T47D human breast cancer cells. T47D cell apoptosis can be triggered by HC-toxin, and this process may not be carried out by directly raising caspase-3/7 activity [2].
In vitro, HC-Toxin demonstrates potent antiproliferative efficacy and induces cell cycle arrest at the G2/M phase in T47D human breast cancer cells in a dose-dependent manner. It evokes apoptosis in T47D cells, and this apoptosis may not be mediated through a direct increase in caspase-3/7 activity. The compound is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin also shows activity against apicomplexan parasites by inhibiting parasite HDACs. |
| ln Vivo |
In vivo, HC-Toxin has been studied for its anticancer effects, though specific in vivo efficacy data are limited. As an HDAC inhibitor, it is expected to show antitumor activity in animal models of cancer by inducing cell cycle arrest, differentiation, and apoptosis in tumor cells. The compound may also have applications in studying parasitic infections due to its activity against apicomplexan HDACs. However, detailed in vivo pharmacokinetic and efficacy data are not extensively reported in the available literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for HC-Toxin typically involve HDAC activity assays using purified recombinant HDAC enzymes or nuclear extracts containing HDAC activity. The assay is performed in 96-well plates with assay buffer (25 mM Tris-HCl pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 0.1 mg/mL BSA). The compound (typically 0.001-100 μM) is incubated with the enzyme and a fluorogenic substrate (e.g., Boc-Lys(Ac)-AMC) at 37°C for 30-60 minutes. The reaction is stopped with developer solution containing trypsin, and fluorescence is measured at excitation 360 nm and emission 460 nm. The IC50 is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for HC-Toxin use T47D human breast cancer cells or other cancer cell lines. Cells are cultured in RPMI-1640 medium with 10% FBS and treated with various concentrations of the compound (typically 0.001-10 μM) for 24-72 hours. Cell proliferation is assessed using MTT or CellTiter-Glo assays. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. Apoptosis is assessed by Annexin V/PI staining, caspase-3/7 activity assays, and Western blotting for cleaved PARP. Histone acetylation (Ac-H3, Ac-H4) is measured by Western blotting.
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| Animal Protocol |
In vivo animal studies with HC-Toxin would typically use mouse xenograft models of cancer. Immunodeficient mice are implanted subcutaneously with cancer cells (e.g., T47D or other breast cancer cells). When tumors reach approximately 100-200 mm3, mice are treated with the compound at doses of 1-10 mg/kg administered intraperitoneally or intravenously, daily or every other day for 2-4 weeks. Tumor volume is measured every 2-3 days. At study termination, tumors are harvested for analysis of histone acetylation, proliferation (Ki67), and apoptosis (cleaved caspase-3).
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HC-Toxin are not extensively reported. The compound is soluble in DMSO at ≥10 mg/mL (22.91 mM). It is a cyclic tetrapeptide with a molecular weight of 436.5, suggesting moderate lipophilicity. The compound is expected to be metabolized by peptidases and hepatic enzymes. Specific PK parameters such as oral bioavailability, half-life, and tissue distribution are not detailed in the available literature. The compound is typically administered via injection in research settings.
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| Toxicity/Toxicokinetics |
The toxicity profile of HC-Toxin is not extensively reported in the available literature. As an HDAC inhibitor, potential toxicities may include effects on normal cell proliferation and differentiation, as well as gastrointestinal and hematological effects. The compound is a mycotoxin and should be handled with care. It is for research use only and not for human therapeutic use. Standard toxicity studies would include acute toxicity in rodents and cytotoxicity assays in normal cell lines.
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| References | |
| Additional Infomation |
HC-Toxin (CAS 83209-65-8) is a cyclic tetrapeptide and potent HDAC inhibitor with an IC50 of 30 nM. It is produced by the fungus Helminthosporium carbonum and has anticancer effects by inducing tumor cell apoptosis. The compound is cell-permeable and used in epigenetics and cancer research. It is not approved for clinical use and is available for research purposes only.
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| Molecular Formula |
C21H32N4O6
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|---|---|
| Molecular Weight |
436.50200
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| Exact Mass |
436.232
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| CAS # |
83209-65-8
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| PubChem CID |
13889849
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
819.2±65.0 °C at 760 mmHg
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| Flash Point |
449.2±34.3 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.562
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| LogP |
-2.99
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
741
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C[C@@H]1C(=O)N[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C(=O)N1)C)CCCCCC(=O)[C@@H]3CO3
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| InChi Key |
GNYCTMYOHGBSBI-SVZOTFJBSA-N
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| InChi Code |
InChI=1S/C21H32N4O6/c1-12-18(27)22-13(2)19(28)24-14(7-4-3-5-9-16(26)17-11-31-17)21(30)25-10-6-8-15(25)20(29)23-12/h12-15,17H,3-11H2,1-2H3,(H,22,27)(H,23,29)(H,24,28)/t12-,13+,14-,15+,17-/m0/s1
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| Chemical Name |
(3S,6R,9S,12R)-6,9-dimethyl-3-[6-[(2S)-oxiran-2-yl]-6-oxohexyl]-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2910 mL | 11.4548 mL | 22.9095 mL | |
| 5 mM | 0.4582 mL | 2.2910 mL | 4.5819 mL | |
| 10 mM | 0.2291 mL | 1.1455 mL | 2.2910 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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