(-)-Parthenolide

N.º de catálogoS2341 Lote:S234110

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Datos técnicos

Fórmula

C15H20O3
Peso molecular 248.32 Número CAS 20554-84-1
Solubilidad (25°C)* In vitro DMSO 50 mg/mL (201.35 mM)
Ethanol 50 mg/mL (201.35 mM)
Water Insoluble
In vivo (Agregue los solventes al producto individualmente y en orden.)
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.
* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción (-)-Parthenolide, un inhibidor de la vía del Nuclear Factor-κB, agota específicamente la proteína HDAC1 sin afectar a otras HDAC de clase I/II; También promueve la ubiquitinación de MDM2 y activa las funciones celulares de p53.
Objetivos
HDAC1 NF-κB MDM2 p53
In vitro

El partenólido (PTL), una lactona sesquiterpénica purificada de los brotes de la matricaria, inhibe la actividad de la peptidasa 7 específica de ubiquitina (USP7) y desubiquitina y estabiliza la β-catenina, que es el factor de transcripción clave de la vía de señalización Wnt, lo que sugiere que el PTL es un agente anticancerígeno prometedor que se dirige a la señalización aberrante USP7/Wnt.
In vivo

El partenólido (PN), un inhibidor de P65, aumenta significativamente el volumen tumoral en un modelo de ratón con xenoinjerto subcutáneo de cáncer gástrico (CG), lo que puede revertirse con gastrina.

Protocolo (de referencia)

Ensayo celular:

[4]
  • Líneas celulares

    HCT116, SW480, HEK293W cells

  • Concentraciones

    2.5, 5.0, 10 μM

  • Tiempo de incubación

    24 h

  • Método

    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.
Estudio en animales:

[5]
  • Modelos animales

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

  • Dosificaciones

    4 mg/kg/day

  • Administración

    --

Referencias

  • 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/

Validación de productos por parte del cliente

<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.

Datos de [ , , 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.

Datos de [ , , J Neuroimmunol, 2017, 305:154-161 ]

Sellecks (-)-Parthenolide Ha sido citado por 27 Publicaciones

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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