| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary targets of Proscillaridin include topoisomerase I and II, and the Na⁺/K⁺ ATPase pump. It is a potent inhibitor of topoisomerase I and II, with IC₅₀ values of 30 nM and 100 nM, respectively. By inhibiting Na⁺/K⁺ ATPase, it enhances intracellular calcium levels, leading to increased cardiac contractility. At high concentrations above 300 nM, it can increase intracellular Ca²⁺ concentration, activate caspase-3, and induce apoptosis in human fibroblasts. It also interacts with the ABCB1 transporter.
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| ln Vitro |
In MCF-7 cells, proscillaridin A (0-160 nM; 48 hours) exhibits antiproliferative effects in a dose- and time-dependent manner [1].
In vitro, Proscillaridin demonstrates potent anticancer activity. In MCF-7 breast cancer cells, it exhibits antiproliferative effects in a dose- and time-dependent manner at concentrations ranging from 0-160 nM. It potently disrupts topoisomerase I and II activity at nanomolar concentrations, triggering cell death and blocking proliferation in glioblastoma cell lines. At concentrations above 300 nM, it can increase intracellular calcium, activate caspase-3, and induce apoptosis in human fibroblasts. It has been reported to target MYC overexpressing leukemia through global loss of lysine acetylation. |
| ln Vivo |
In vivo, Proscillaridin has been investigated for its cardiovascular and anticancer properties. As a cardiac glycoside, it has been used in the research of congestive heart failure and arrhythmias. Its mechanism involves inhibiting the Na⁺/K⁺ ATPase pump, which increases intracellular calcium and contractility. Its anticancer potential is suggested by its potent topoisomerase inhibition and cytotoxic effects on cancer cell lines. Further in vivo studies are needed to fully characterize its efficacy and safety in different disease models.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for Proscillaridin involve assessing its inhibition of topoisomerase I and II. The compound's activity can be measured using a DNA relaxation assay for topoisomerase I, where the inhibition of enzyme-mediated relaxation of supercoiled DNA is quantified. For topoisomerase II, a decatenation assay can be used. IC₅₀ values are determined from dose-response curves. Its interaction with the Na⁺/K⁺ ATPase pump can be studied by measuring the inhibition of ATP hydrolysis or rubidium uptake. These protocols are for reference only.
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| Cell Assay |
In vitro cell-based assays for Proscillaridin evaluate its antiproliferative and cytotoxic effects. Cancer cell lines such as MCF-7 (breast cancer) or glioblastoma cells are cultured in appropriate media and treated with various concentrations of the compound for 24-72 hours. Cell viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. Apoptosis is measured using Annexin V/PI staining or caspase-3/7 activity assays. Cell cycle analysis is performed using propidium iodide staining and flow cytometry. Intracellular calcium levels can be measured using fluorescent calcium indicators.
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| Animal Protocol |
In vivo animal studies for Proscillaridin would typically involve models of heart failure or cancer. For heart failure, animal models like the rat model of myocardial infarction could be used to assess the compound's inotropic effects. For cancer, xenograft models bearing tumors such as glioblastoma or leukemia could be employed. The compound would be administered via intraperitoneal or intravenous injection. Endpoints would include tumor growth inhibition, survival, and cardiac function parameters. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Proscillaridin are not fully detailed in the provided literature. It has a molecular weight of 530.6 g/mol. As a cardiac glycoside, it is typically administered parenterally due to poor oral bioavailability. The compound's half-life, distribution, and elimination would need to be determined in preclinical studies. It is soluble in DMSO. For research use, it should be stored under appropriate conditions.
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| Toxicity/Toxicokinetics |
The toxicity profile of Proscillaridin is consistent with that of cardiac glycosides, which have a narrow therapeutic index. Overdose can lead to cardiac arrhythmias and other serious side effects. The compound is classified for research use only and not for human consumption. At high concentrations (>300 nM), it can induce apoptosis in human fibroblasts. Standard safety precautions for handling potent bioactive compounds should be followed.
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| References | |
| Additional Infomation |
Proto-onyrosin is an organic molecular entity. It is a cardiac glycoside derived from plants of the genus Scilla and Scilla maritima. Studies have shown that proto-onyrosin possesses potential cytotoxic and anticancer properties, evidenced by its ability to effectively interfere with the activity of topoisomerases I and II at nanomolar concentrations, and to induce cell death and inhibit cell proliferation in glioblastoma cell lines. Proto-onyrosin has also been reported to be found in Drimia indica, with relevant data available. It is a cardiac glycoside isolated from Scilla maritima var. alba.
Additional information: Proscillaridin has the CAS number 466-06-8. Its molecular formula is C₃₀H₄₂O₈ and its molecular weight is 530.6 g/mol. The compound is also known as Talusin. It is a cardiotonic glycoside that inhibits topoisomerase I and II with IC₅₀s of 30 nM and 100 nM, respectively. Proscillaridin is a research tool for studying topoisomerase inhibition, cardiac contractility, and anticancer mechanisms. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C30H42O8
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|---|---|
| Molecular Weight |
530.6497
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| Exact Mass |
530.287
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| CAS # |
466-06-8
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| PubChem CID |
5284613
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
716.7±60.0 °C at 760 mmHg
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| Melting Point |
233ºC
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| Flash Point |
232.6±26.4 °C
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| Vapour Pressure |
0.0±5.2 mmHg at 25°C
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| Index of Refraction |
1.620
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
38
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)O[C@H]2CC[C@@]3([C@H]4CC[C@@]5([C@H](CC[C@@]5([C@@H]4CCC3=C2)O)C6=COC(=O)C=C6)C)C)O)O)O
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| InChi Key |
MYEJFUXQJGHEQK-ALRJYLEOSA-N
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| InChi Code |
InChI=1S/C30H42O8/c1-16-24(32)25(33)26(34)27(37-16)38-19-8-11-28(2)18(14-19)5-6-22-21(28)9-12-29(3)20(10-13-30(22,29)35)17-4-7-23(31)36-15-17/h4,7,14-16,19-22,24-27,32-35H,5-6,8-13H2,1-3H3/t16-,19-,20+,21-,22+,24-,25+,26+,27-,28-,29+,30-/m0/s1
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| Chemical Name |
5-[(3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-1,2,3,6,7,8,9,11,12,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-one
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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 Vitro) |
DMSO : ~100 mg/mL (~188.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.71 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 25.0 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: ≥ 2.5 mg/mL (4.71 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8845 mL | 9.4224 mL | 18.8448 mL | |
| 5 mM | 0.3769 mL | 1.8845 mL | 3.7690 mL | |
| 10 mM | 0.1884 mL | 0.9422 mL | 1.8845 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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