Helichrysetin
Based on 1 Customer Validation
Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity.
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 62014-87-3
- Formula: C16H14O5
- Molecular Weight:286.28
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>50 μM
Compound: 11a
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Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
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[PMID: 25629304] |
| HeLa | IC50 |
48.1 μM
Compound: 11a
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Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
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[PMID: 25629304] |
| HeLa | IC50 |
5.2 μM
Compound: 12, Helichrysetin
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Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
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[PMID: 18343123] |
| HepG2 | IC50 |
40.2 μM
Compound: 11a
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Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
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[PMID: 25629304] |
| HT-1080 | ED50 |
40.1 μM
Compound: 9
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Antiproliferative activity against human HT1080 cells by MTT assay
Antiproliferative activity against human HT1080 cells by MTT assay
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[PMID: 11277741] |
| Macrophage | IC50 |
21.7 μM
Compound: 28
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Toxicity against BALB/c mouse macrophage by MTT assay
Toxicity against BALB/c mouse macrophage by MTT assay
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[PMID: 19962891] |
Helichrysetin (0-100 μM, 48 h) inhibits the development of ductal carcinoma in situ (DCIS) by targeting DNA inhibitor 2 (ID2) [2].
Helichrysetin (5-20 μg/mL, 48 h) can block the cell cycle and induce apoptosis in A549 human lung cancer cells[2].
Helichrysetin (10-40 μM, 48 h) inhibits the growth of gastric cancer cells by targeting mTOR/p70S6K/c-Myc/ PDHK1-mediated energy metabolic reprogramming of cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29, A549, MCF-7, and Ca Ski
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Concentration:1.56, 3.13, 6.25, 12.5, 25, 50, 100 μg/mL
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Incubation Time:72 h
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Result:Inhibited cell growth in a dose-dependent manner. IC50 for A549, Ca Ski, HT29, MCF-7 was 50.72 ± 1.26 μM (14.52 ± 0.36 μg/mL), 31.02 ± 0.45 μM (8.88 ± 0.13 μg/mL), 102.94 ± 2.20 μM (29.47 ± 0.63 μg/mL) and 97.35 ± 1.71 μM (27.87 ± 0.49 μg/mL).
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Cell Line:A549
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Concentration:5, 15, 20 μg/mL
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Incubation Time:24-72 h
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Result:The population of early apoptotic cells increased from 2.65 ± 0.31% (control) to 2.78 ± 0.21%, 14.98 ± 0.79%, and 28.55 ±1.19%. Caused accumulation of cells in S phase, occurring simultaneously with the significant reduction of cell percentage in G0/G1 phase with 15 and 20 μg/mL.
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Cell Line:MGC803
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Concentration:10, 20 40 μM
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Incubation Time:24 h
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Result:Increased the protein expression of cleaved caspase 3 (20 and 40 μM) and reduced protein expression of Bcl-2 (40 μM), but had no significant effect on the protein expression of Bax.
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Cell Line:MGC803
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Concentration:10, 20 40 μM
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Incubation Time:24 h
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Result:Reduced the mRNA and protein expression of PDHK1 and LDHA but only decreased the mRNA level of LDHB. Decreased the protein expression of pyruvate dehydrogenase phosphatase (PDP) 2 and the ratio of p-PDHA1/PDHA1. Increased the expression levels of Nrf2, HO-1, and NQO-1 and reduced Keap1. Inhibited the phosphorylation of PI3K, Akt, mTOR, and P70S6K.
Helichrysetin (3, 10, 30 mg/kg, Intraperitoneal injection) can inhibit tumor growth in a mouse model of gastric cancer cell transplantation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MGC803 cell-xenografted mouse model[3]
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Dosage:3, 10, 30 mg/kg
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Administration:i.p.
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Result:Decreased the tumor size and weight without an obvious effect on body weight in nude mice. Reduced the expression of Ki67 and increased the number of apoptotic cells in tumor tissues.
Chemical Information
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CAS No. 62014-87-3
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Appearance Solid
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Molecular Weight 286.28
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Formula C16H14O5
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Color White to yellow
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SMILES
O=C(C1=C(OC)C=C(O)C=C1O)/C=C/C2=CC=C(O)C=C2
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (174.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Liu Y, et al. ID2 and GJB2 promote early-stage breast cancer progression by regulating cancer stemness. Breast Cancer Res Treat. 2019 May;175(1):77-90. [Content Brief]
[2]. Ho YF, et al. Induction of apoptosis and cell cycle blockade by helichrysetin in a549 human lung adenocarcinoma cells. Evid Based Complement Alternat Med. 2013;2013:857257. [Content Brief]
[3]. Wang P, et al. Helichrysetin inhibits gastric cancer growth by targeting c-Myc/PDHK1 axis-mediated energy metabolism reprogramming. Acta Pharmacol Sin. 2022 Jun;43(6):1581-1593. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4931 mL | 17.4654 mL | 34.9308 mL | 87.3271 mL |
| 5 mM | 0.6986 mL | 3.4931 mL | 6.9862 mL | 17.4654 mL | |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.4931 mL | 8.7327 mL | |
| 15 mM | 0.2329 mL | 1.1644 mL | 2.3287 mL | 5.8218 mL | |
| 20 mM | 0.1747 mL | 0.8733 mL | 1.7465 mL | 4.3664 mL | |
| 25 mM | 0.1397 mL | 0.6986 mL | 1.3972 mL | 3.4931 mL | |
| 30 mM | 0.1164 mL | 0.5822 mL | 1.1644 mL | 2.9109 mL | |
| 40 mM | 0.0873 mL | 0.4366 mL | 0.8733 mL | 2.1832 mL | |
| 50 mM | 0.0699 mL | 0.3493 mL | 0.6986 mL | 1.7465 mL | |
| 60 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4555 mL | |
| 80 mM | 0.0437 mL | 0.2183 mL | 0.4366 mL | 1.0916 mL | |
| 100 mM | 0.0349 mL | 0.1747 mL | 0.3493 mL | 0.8733 mL |