| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Bax; Mcl-1; c-FLIP; COX-2
Jaceosidin targets multiple pathways including apoptosis regulation through Bax activation and Mcl-1/c-FLIP downregulation. It also modulates inflammatory pathways by inhibiting NF-κB activation and COX-2 expression. Jaceosidin blocks ERK-1 and ERK-2 phosphorylation in human mammary epithelial cells, thereby inhibiting phorbol ester-induced COX-2 expression. As a flavonoid, it may interact with multiple cellular targets including kinases, transcription factors, and enzymes involved in inflammation and cell survival. The compound's mechanism involves both pro-apoptotic and anti-inflammatory signaling modulation. |
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| ln Vitro |
After 24 hours of treatment, human kidney carcinoma Caki cells undergo disinfection induced by jaceosidin (30, 50, and 75 μM), but normal cells experience no discernible effects [1]. via suppressing NF-κB and/or Sp1 regulatory activity, Jaceosidin (75 μM) lowers MMP levels via activating Bax and releases cytochromes into Jaceosidin-induced cells to participate in Mcl-1, c-FLIP-mediated transcription [1]. In the cytoplasm of HES and HESC, jaceosidin is active [1]. After 48 hours of treatment, the inhibitory activity (IC50 values were 52.68 and 55.10 μM, respectively) and cytotoxicity (IC50 values were 70.54 and 147.14 μM, respectively) to Hec1 A and KLE were increased [2].
In vitro, Jaceosidin induces apoptosis in cancer cells by activating Bax and downregulating Mcl-1 and c-FLIP expression. It exhibits anti-proliferative activity in many cancer cell lines. Jaceosidin reduces the levels of inflammatory factors and inhibits COX-2 expression, demonstrating anti-inflammatory activity. The compound activates NF-κB while also inhibiting COX-2 expression. It blocks ERK-1 and ERK-2 phosphorylation in human mammary epithelial cells, thereby inhibiting phorbol ester-induced COX-2 expression. Jaceosidin exhibits antioxidant and anti-allergic activities. |
| ln Vivo |
Jaceosidin (10 and 20 mg/kg, once day for three days), used as a face increases in the amount of leukocytes and protein levels in nozzle coat exudates caused by burns carrageenan [3]. Jaceosidin (20 mg/kg po every two days, hourly) lessens the volume of edema in paws that are edematous [3]. /kg, po) suppresses NF-κB activator and COX-2 expression in mice [3]. Male BALB/c mice aged 5 weeks, weighing 23–26 g [3]
In vivo, Jaceosidin has anti-cancer and anti-inflammatory effects. By activating Bax and downregulating Mcl-1 and c-FLIP, the compound induces apoptosis in tumor cells. Its anti-inflammatory effects are mediated through inhibition of NF-κB activation and COX-2 expression. However, specific in vivo efficacy data from animal models is not detailed in the available sources. Jaceosidin shows promise as a therapeutic agent for cancer and inflammatory diseases. |
| Enzyme Assay |
For apoptosis inducers and anti-inflammatory compounds, standard cell-free assays include enzyme activity assays for COX-2 inhibition and NF-κB DNA binding assays (EMSA or ELISA-based). The compound's ability to modulate these targets can be assessed using purified enzymes or nuclear extracts. Antioxidant activity can be measured using DPPH, ABTS, or FRAP assays.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Hec1A, KLE, HES and HESC Cell Tested Concentrations: 3.125, 6.25, 12.5, 25, 50 and 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated cytostatic activity against HES and HESC cells, IC50 is 52.68 and 55.10 μM, less cytotoxic Hec1 A and KLE (IC50, 70.54, 147.14 μM). For apoptosis-inducing compounds, standard cellular assays involve treatment of cancer cell lines with the test compound for 24-72 hours. Apoptosis is assessed by Annexin V/PI staining, caspase activity assays, and DNA fragmentation. Bax, Mcl-1, and c-FLIP expression is measured by western blot. COX-2 expression and NF-κB activation are assessed by western blot or qPCR. Cell viability is measured using MTT or CellTiter-Glo assays. |
| Animal Protocol |
Animal/Disease Models: 5weeks old male balb/c (Bagg ALBino) mouse (23-26 g)[3]
Doses: 10 and 20 mg/kg Route of Administration: P.O. one time/day for 3 days Experimental Results:diminished the volumes of exudates (inflammatory markers), cell number and protein levels. Inhibited TNF-α by 46.7% and 50.8%, IL-1β by 46.0% and 44.7%, and PGE2 by 21.7% and 16.9%, respectively, at 20 mg/kg. Blocked COX-2 expression and NF-κB activation. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (180-200 g)[3] Doses: 20 mg/kg Route of Administration: P.O., for 2 hour Experimental Results:diminished hind paw edema volume by 27.1% at 1 h, and 24.0% at 2 h, respectively. For in vivo evaluation of anti-cancer compounds, standard animal models include tumor xenograft models using cancer cell lines sensitive to apoptosis induction. The compound is typically administered orally or intraperitoneally for 2-4 weeks. Tumor growth, apoptosis markers, and inflammatory markers are assessed. For anti-inflammatory studies, models of acute or chronic inflammation are used. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Jesseoglycoside is a known human metabolite of uropatilol. Detailed pharmacokinetic data for Jaceosidin is not provided in the available sources. The compound has a molecular weight of approximately 314.29 and formula C16H12O6 (trihydroxyflavone). As a flavonoid with moderate lipophilicity, it would be expected to have reasonable oral absorption and distribution. Comprehensive pharmacokinetic studies would be required for therapeutic development. |
| Toxicity/Toxicokinetics |
Detailed toxicology data for Jaceosidin is not provided in the available sources. As a naturally occurring flavonoid found in medicinal herbs of the genus Artemisia, it may have a favorable safety profile at moderate doses. However, comprehensive toxicological evaluation would be required for therapeutic development. The compound is for research use only and not for therapeutic applications.
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| References |
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| Additional Infomation |
Jaceosidin is a trihydroxyflavonoid with hydroxyl groups at the 5', 7', and 4' positions and methoxy groups at the 3' and 6' positions. It was isolated from Salvia tomentosa and Artemisia asiatica and possesses anti-allergic, anti-inflammatory, and apoptosis-inducing activities. It can function as a metabolite, anti-inflammatory agent, apoptosis inducer, anti-allergic agent, and antitumor agent. It is a trihydroxyflavonoid and a dimethoxyflavonoid. Jaceosidin has also been reported to exist in Disynaphia multicrenulata, Stylidocleome brachycarpa, and several other organisms with relevant data.
Jaceosidin is also known as 4'-Demethyleupatilin and is a trihydroxyflavone that exhibits anti-allergic, anti-inflammatory, and apoptosis-inducing activities. It is found in the medicinal herbs of the genus Artemisia. The compound activates Bax and down-regulates Mcl-1 and c-FLIP expression. No regulatory approval has been identified. |
| Molecular Formula |
C17H14O7
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|---|---|
| Molecular Weight |
330.2889
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| Exact Mass |
330.073
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| Elemental Analysis |
C, 61.82; H, 4.27; O, 33.91
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| CAS # |
18085-97-7
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| Related CAS # |
18085-97-7
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| PubChem CID |
5379096
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
619.0±55.0 °C at 760 mmHg
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| Flash Point |
232.0±25.0 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.671
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
505
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(=C([H])C(C2C(=C(C(=C([H])C1=2)O[H])OC([H])([H])[H])O[H])=O)C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])[H])O[H]
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| InChi Key |
GLAAQZFBFGEBPS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14O7/c1-22-13-5-8(3-4-9(13)18)12-6-10(19)15-14(24-12)7-11(20)17(23-2)16(15)21/h3-7,18,20-21H,1-2H3
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| Chemical Name |
5,7-dihydroxy-2-(4-hydroxy-3-methoxyphenyl)-6-methoxychromen-4-one
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| Synonyms |
Jaceosidin
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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: 66~125 mg/mL (199.8~378.5 mM)
Ethanol: 6~7.1 mg/mL (18.2~21.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.30 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 (6.30 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.30 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 | 3.0276 mL | 15.1382 mL | 30.2764 mL | |
| 5 mM | 0.6055 mL | 3.0276 mL | 6.0553 mL | |
| 10 mM | 0.3028 mL | 1.5138 mL | 3.0276 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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