| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Active oxygen (reactive oxygen species) is involved in the induction of apoptosis caused by rhapontin in KATO III cells. [1]
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| ln Vitro |
Rhapontin inhibited the proliferation of human stomach cancer KATO III cells in a dose-dependent manner. At 50 μM, inhibition was 29.3%; at 100 μM, 56.8%; and at 200 μM, 98.6% after 3 days of treatment. [1]
Morphological changes characteristic of apoptosis, including formation of apoptotic bodies, were observed in KATO III cells treated with 200 μM rhapontin for 3 days. [1] Rhapontin induced DNA fragmentation into oligonucleosomal-sized fragments (DNA laddering) in KATO III cells in a concentration-dependent manner (from 50 to 200 μM) and time-dependent manner (from 1 to 3 days). [1] The antioxidant N-acetyl-L-cysteine (5 mM, pre-incubated for 2 hours) suppressed the DNA fragmentation induced by 200 μM rhapontin in KATO III cells after 3 days of co-treatment. [1] In contrast, rhapontin did not induce apoptosis in normal human lymphocytes prepared from healthy volunteers. [1] |
| Cell Assay |
Human stomach cancer KATO III cells were cultured in 45% RPMI-1640 medium with 45% Eagle's minimal essential medium containing 10% heat-inactivated fetal bovine serum, penicillin G (50 IU/ml), and streptomycin (50 μg/ml) at 37°C under humidified 95% air – 5% CO₂ atmosphere, and passaged every 4 days. Exponentially growing cells were seeded at 4–5 × 10⁵ cells/ml in culture flasks and cultivated with vehicle (50% ethanol) or rhapontin for 1–3 days. Viable cell numbers were evaluated using the trypan blue dye exclusion method. [1]
For morphological observation, KATO III cells were seeded at 4–5 × 10⁵ cells/ml and cultivated with vehicle or rhapontin for 3 days. Cell morphology was examined under an epifluorescence microscope with a cooled CCD camera digital imaging system. [1] For DNA fragmentation assay, KATO III cells were seeded at 4–5 × 10⁵ cells/ml and cultivated with vehicle, rhapontin, or resveratrol for 1–3 days. Cells were pelleted by slow centrifugation, and DNA was isolated from cell pellets. Equivalent amounts of DNA (2 μg) were loaded into wells of 2% agarose gel and electrophoresed in 40 mM Tris-acetic acid (pH 7.5) containing 2 mM EDTA. [1] To assess the effect of an antioxidant, KATO III cells were pre-incubated for 2 hours with 5 mM N-acetyl-L-cysteine, then rhapontin (200 μM) was added, and cells were cultured for 3 days. DNA was then isolated and analyzed by agarose gel electrophoresis as described. [1] Normal human lymphocytes were prepared from heparinized blood diluted with physiological saline (1:1) layered over lymphocyte separation medium, centrifuged at 400×g for 20 min at room temperature. The lymphocyte layer was washed with phosphate-buffered saline (pH 7.5) and centrifuged at 260×g for 10 min. Cells were suspended in RPMI-1640 medium containing 10% FCS and 2% phytohemagglutinin-M, then cultivated with vehicle or rhapontin for 3 days. [1] |
| Toxicity/Toxicokinetics |
Rhapontin did not induce apoptosis in normal human lymphocytes prepared from healthy volunteers, indicating a lack of apoptotic effect on these normal cells under the tested conditions. [1]
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| References | |
| Additional Infomation |
Trans-emodin is a type of emodin with a trans configuration of its double bonds. It possesses various pharmacological activities, including antitumor, anti-inflammatory, lipid-lowering, and neuroprotective effects. It can function as an anti-inflammatory agent, a plant metabolite, a neuroprotective agent, an EC 2.3.1.85 (fatty acid synthase) inhibitor, an antitumor agent, an apoptosis inducer, an angiogenesis inhibitor, a hypoglycemic agent, an anti-allergic agent, and a lipid-lowering drug. Emodin has been reported to be found in plants of the genus Rheum (such as Rheum likiangense and Rheum franzenbachii) and other organisms with relevant data.
Rhapontin is a component of rhubarb (Rheum officinale Baillon). Its chemical structure contains a stilbene moiety. Other compounds isolated from rhubarb such as physcion, sennidine A and B, sennoside A and B, chrysophanol, emodin, anthrone, and rhein did not induce apoptosis in KATO III cells, whereas resveratrol (also containing a stilbene moiety) did induce apoptosis. This suggests that the stilbene moiety is essential for apoptosis induction. [1] The mechanism involves active oxygen species, as the antioxidant N-acetyl-L-cysteine suppressed DNA fragmentation induced by rhapontin. Active oxidants are proposed to work as apoptosis-inducing signal transfer substances, possibly through non-caspase-dependent cascades. [1] The study suggests that rhapontin might exert antitumor activity by triggering apoptosis in stomach cancer cells, without altering healthy cells (as observed in normal lymphocytes). [1] |
| Molecular Formula |
C21H24O9
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|---|---|
| Molecular Weight |
420.4099
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| Exact Mass |
420.142
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| Elemental Analysis |
C, 66.27; H, 7.60; N, 2.58; O, 17.66; S, 5.90
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| CAS # |
155-58-8
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| Related CAS # |
1314795-11-3
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| PubChem CID |
637213
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| Appearance |
Yellow to brown solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
749.3±60.0 °C at 760 mmHg
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| Melting Point |
236-240ºC
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| Flash Point |
406.9±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.711
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| LogP |
0.68
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
559
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1[C@]([H])([C@@]([H])([C@]([H])([C@@]([H])([C@@]1([H])C([H])([H])O[H])O[H])O[H])O[H])OC1C([H])=C(C([H])=C(/C(/[H])=C(\[H])/C2C([H])=C([H])C(=C(C=2[H])O[H])OC([H])([H])[H])C=1[H])O[H]
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| InChi Key |
GKAJCVFOJGXVIA-DXKBKAGUSA-N
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| InChi Code |
InChI=1S/C21H24O9/c1-28-16-5-4-11(8-15(16)24)2-3-12-6-13(23)9-14(7-12)29-21-20(27)19(26)18(25)17(10-22)30-21/h2-9,17-27H,10H2,1H3/b3-2+/t17-,18-,19+,20-,21-/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[3-hydroxy-5-[(E)-2-(3-hydroxy-4-methoxyphenyl)ethenyl]phenoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
Radalbuvir; GS-9669; GS9669; GS 9669
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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: 84~250 mg/mL (199.8~594.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.3786 mL | 11.8932 mL | 23.7863 mL | |
| 5 mM | 0.4757 mL | 2.3786 mL | 4.7573 mL | |
| 10 mM | 0.2379 mL | 1.1893 mL | 2.3786 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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