(-)-Parthenolide

Catalogusnr.S2341 Batch:S234109

Afdrukken

Technische gegevens

Formule

C15H20O3
Molecuulgewicht 248.32 CAS-nr. 20554-84-1
Oplosbaarheid (25°C)* In vitro DMSO 50 mg/mL (201.35 mM)
Ethanol 50 mg/mL (201.35 mM)
Water Insoluble
In Vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 2.500mg/ml (10.07mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving (-)-Parthenolide, een remmer van de Nuclear Factor-κB Pathway, vermindert specifiek HDAC1-eiwit zonder andere klasse I/II HDAC's te beïnvloeden; het bevordert ook de ubiquitinatie van MDM2 en activeert p53 cellulaire functies.
Doelen
HDAC1 NF-κB MDM2 p53
In vitro

Parthenolide (PTL), een sesquiterpeenlacton gezuiverd uit de scheuten van moederkruid, remt de ubiquitin-specifieke peptidase 7 (USP7) activiteit en deubiquitineert en stabiliseert β-catenine, de belangrijkste transcriptionele factor van de Wnt-signaleringsroute, wat suggereert dat PTL een veelbelovend middel tegen kanker is dat gericht is op aberrante USP7/Wnt-signalering.
In Vivo

Parthenolide (PN), een P65-remmer, verhoogt significant de tumorgrootte in een subcutaan xenograft maagkanker (GC) muismodel, wat kan worden omgekeerd door gastrine.

Protocol (uit referentie)

Celassay:

[4]
  • Cellijnen

    HCT116, SW480, HEK293W cells

  • Concentraties

    2.5, 5.0, 10 μM

  • Incubatietijd

    24 h

  • Methode

    To confirm PTL as a Wnt signaling inhibitor, HEK293W cells are seeded in 96-well plates with three repeats and treated with PTL for 24 h. HCT116 and SW480 cells are seeded in 96-well plates and then transfected as follows: Wnt/β-catenin signaling responsive Firefly luciferase reporter plasmid SuperTOPFlash (80 ng/well) and Renilla reporter plasmid (8 ng/well). After 3-h transfection, cells are exposed to various concentrations of PTL for 24 h and then lysed. Both Firefly and Renilla luciferase activities are measured using the Dual-Luciferase Reporter Assay kit.
Dierstudie:

[5]
  • Dierlijke modellen

    Female athymic BALB/c nude mice of xenograft gastric cancer (GC) model

  • Doseringen

    4 mg/kg/day

  • Toediening

    --

Referenties

  • https://pubmed.ncbi.nlm.nih.gov/17656318/
  • https://pubmed.ncbi.nlm.nih.gov/11961112/
  • https://pubmed.ncbi.nlm.nih.gov/19276167/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076227/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5987590/

Klantproductvalidatie

<p> G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells</p>

, , Harvard University, 2014.

Induction of apoptosis by HDAC and DNMT1 inhibitors. a-c/ Membrane permeability apoptosis and necrosis assays were performed in which apoptotic cells positively stain for YO-PRO1 and necrotic cellspositively stain for PI. Cells undergoing late apoptosis positively stain for both YO-PRO1 and PI. Nuclei were counterstained with Hoechst 33342. Apoptosis assay results are shown for Daoy cells that were exposed to: a/DMSO, b/2 μMparthenolide and c/2 μMparthenolide plus 33 nM 5-azadC, each for 24 h and 48 h, as indicated. d–f Annexin Vapoptosis assays of Daoy cells exposed to (d) DMSO, (e) 2 μMparthenolide and (f) 2 μM parthenolide plus 33 nM 5-aza-dC for 24 h. Nuclei were counterstained with DAPI.

Gegevens van [ , , Cell Oncol (Dordr), 2017, 40(3):263-279 ]

PAR inhibited the production of TNF-α and IL-17 in vitro in a dose dependent manner. Lymph node MNCs harvested from EAN rats on day 8 p.i. were cultured in the presence of BPM and a series of concentrations of PAR. 72 h later, culture supernatants were collected and the levels of TNF-α and IL-17 were detected by ELISA. The results are expressed as mean ± SD (*p < 0.05, **p < 0.01). Data represented three experiments.

Gegevens van [ , , J Neuroimmunol, 2017, 305:154-161 ]

Sellecks (-)-Parthenolide Is geciteerd door 27 Publicaties

Ketogenic diet and β-hydroxybutyrate inhibit HDAC1 to preserve vascular smooth muscle cell function in thoracic aortic aneurysm [ J Adv Res, 2025, S2090-1232(25)00353-4] PubMed: 40398746
Synergistic activity of S63845 and parthenolide to overcome acquired resistance to MEK1/2 inhibitor in melanoma cells: Mechanisms and therapeutic potential [ Biomed Pharmacother, 2025, 188:118183] PubMed: 40424823
Development of translational read-through-inducing drugs as novel therapeutic options for patients with Fanconi anemia [ Cell Death Discov, 2025, 11(1):286] PubMed: 40544182
TNFSF14-HVEM/LTβR Exacerbates Keratinocyte Abnormalities and IMQ-Induced Psoriatic Skin Inflammation via Activating NF-κB/TWIST1 Signalling Pathway [ J Cell Mol Med, 2025, 29(15):e70774] PubMed: 40768619
Astaxanthin suppresses the malignant behaviors of nasopharyngeal carcinoma cells by blocking PI3K/AKT and NF-κB pathways via miR-29a-3p [ Genes Environ, 2024, 46(1):10] PubMed: 38649975
Parthenolide Targets NLRP3 to Treat Inflammasome-Related Diseases [ Int Immunopharmacol, 2023, 119:110229.] PubMed: 37167640
Connexin43 is associated with the progression of clear cell renal carcinoma and is regulated by tangeretin to sygergize with tyrosine kinase inhibitors [ Transl Oncol, 2023, 35:101712] PubMed: 37354638
Histone deacetylase 1 controls cardiomyocyte proliferation during embryonic heart development and cardiac regeneration in zebrafish [ PLoS Genet, 2021, 17(11):e1009890] PubMed: 34723970
Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia [ Cancer Cell, 2020, 38(6):872-890.e6] PubMed: 33217342
Lack of FGF21 promotes NASH-HCC transition via hepatocyte-TLR4-IL-17A signaling [ Theranostics, 2020, 10(22):9923-9936] PubMed: 32929325

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.