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| 1mg |
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| 5mg |
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| Targets |
Helichrysetin targets ID2 (DNA binding inhibitor 2), a protein that inhibits DNA binding of transcription factors. By inhibiting ID2, Helichrysetin modulates gene expression and cell proliferation. The compound also modulates mTOR/p70S6K/c-Myc/PDHK1-mediated energy metabolic reprogramming of cancer cells. Additionally, Helichrysetin may bind to TNFR1 or its adaptor molecules to inhibit TAK1 activation and synergistically promote apoptosis by inhibiting TNF-α-induced TAK1/IKK/NF-κB and TAK1/EGFR signaling pathways.
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| ln Vitro |
In vitro, Helichrysetin (0-100 μM) demonstrates strong inhibitory activity against cell growth and can induce apoptosis in A549 cells. It has cytotoxic effects on four selected cancer cell lines: A549, MCF-7, Ca Ski, and HT-29. The compound has anti-tumor and antioxidant activities and modulates mTOR/p70S6K/c-Myc/PDHK1-mediated energy metabolic reprogramming of cancer cells.
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| ln Vivo |
In vivo studies on Helichrysetin are limited. As an ID2 inhibitor with anti-tumor activity, it would be expected to be evaluated in animal models of cancer. The compound's effects on tumor growth, apoptosis, and metabolic reprogramming would be assessed in xenograft models.
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| Enzyme Assay |
Cell-free biochemical assays for Helichrysetin involve measuring its effects on ID2 activity and signaling pathways. The compound's ability to inhibit ID2 function can be assessed using DNA binding assays or by measuring the activity of ID2-regulated transcription factors. Its effects on TNFR1 signaling and TAK1/IKK/NF-κB activation can be assessed using kinase assays and electrophoretic mobility shift assays (EMSAs).
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| Cell Assay |
In vitro cellular assays for Helichrysetin use various cancer cell lines, including A549, MCF-7, Ca Ski, and HT-29. Cells are treated with various concentrations of Helichrysetin (0-100 μM), and cell viability is measured using MTT or CCK-8 assays. Apoptosis is assessed by flow cytometry or by measuring caspase activity. The compound's effects on signaling pathways, including mTOR/p70S6K/c-Myc/PDHK1 and TNF-α-induced NF-κB and EGFR signaling, are assessed by Western blot.
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| Animal Protocol |
In vivo animal studies for Helichrysetin would typically use mouse xenograft models of cancer. Immunodeficient mice are inoculated with cancer cells, and when tumors reach a certain size, animals are randomized to receive Helichrysetin or vehicle control. The compound is administered via intraperitoneal injection or oral gavage. Tumor growth is monitored by caliper measurements. At the end of the study, tumors are collected for analysis of signaling pathways, apoptosis, and metabolic reprogramming.
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| ADME/Pharmacokinetics |
Helichrysetin has a molecular formula of C₁₆H₁₄O₅ and a molecular weight of 286.28. It is soluble in DMSO (~50 mg/mL). The compound requires protection from light during transportation and storage. It should be stored as a powder at -20°C for 3 years and in solution at -80°C for 6 months. It is stable at room temperature for a few days during shipping.
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| Toxicity/Toxicokinetics |
Helichrysetin is a naturally occurring chalcone extracted from Helichrysum odoratissimum. It is an ID2 inhibitor that suppresses the formation of DCIS. The compound has strong inhibitory activity against cell growth, induces apoptosis in A549 cells, and has cytotoxic effects on A549, MCF-7, Ca Ski, and HT-29 cell lines. It has anti-tumor and antioxidant activities and modulates mTOR/p70S6K/c-Myc/PDHK1-mediated energy metabolic reprogramming. Helichrysetin is for research use only and not for human therapeutic use.
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| References |
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| Additional Infomation |
Helichrysetin is a type of chalcone compound. It has been reported to exist in ginger species such as Zingiber officinale, Zingiber officinale hainanense, and other organisms with relevant data.
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| Molecular Formula |
C16H14O5
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|---|---|
| Molecular Weight |
286.28
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| Exact Mass |
286.084
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| CAS # |
62014-87-3
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| PubChem CID |
6253344
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| Appearance |
White to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
532.0±50.0 °C at 760 mmHg
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| Flash Point |
201.0±23.6 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
3.08
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
373
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=CC(=C1C(=O)/C=C/C2=CC=C(C=C2)O)O)O
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| InChi Key |
OWGUBYRKZATRIT-QPJJXVBHSA-N
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| InChi Code |
InChI=1S/C16H14O5/c1-21-15-9-12(18)8-14(20)16(15)13(19)7-4-10-2-5-11(17)6-3-10/h2-9,17-18,20H,1H3/b7-4+
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| Chemical Name |
(E)-1-(2,4-dihydroxy-6-methoxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
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| Synonyms |
2-Propen-1-one.; Helichrysetin
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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) |
DMSO : ~50 mg/mL (~174.65 mM)
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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 | 3.4931 mL | 17.4654 mL | 34.9308 mL | |
| 5 mM | 0.6986 mL | 3.4931 mL | 6.9862 mL | |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.4931 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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