(-)-Parthenolide

카탈로그 번호S2341 배치:S234107

인쇄

기술 자료

화학식

C15H20O3
분자량 248.32 CAS 번호 20554-84-1
용해도 (25°C)* 시험관 내(In vitro) DMSO 49 mg/mL (197.32 mM)
Ethanol 49 mg/mL (197.32 mM)
Water Insoluble
생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)
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/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 Nuclear Factor-κB 경로 억제제인 (-)-Parthenolide는 다른 class I/II HDAC에는 영향을 미치지 않으면서 HDAC1 단백질을 특이적으로 고갈시킵니다. 또한 MDM2의 유비퀴틴화를 촉진하고 p53 세포 기능을 활성화합니다.
표적
HDAC1 NF-κB MDM2 p53
시험관 내(In vitro)

피버퓨(feverfew) 새싹에서 정제된 세스퀴테르펜 락톤인 파르테놀리드(PTL)는 유비퀴틴 특이적 펩티다아제 7(USP7) 활성을 억제하고 Wnt 신호 전달 경로의 핵심 전사 인자인 β-카테닌을 탈유비퀴틴화하고 안정화하여 PTL이 비정상적인 USP7/Wnt 신호 전달을 표적으로 하는 유망한 항암제임을 시사합니다.
생체 내(In Vivo)

P65 억제제인 파르테놀리드(PN)는 피하 이종이식 위암(GC) 마우스 모델에서 종양 부피를 유의하게 증가시키며, 이는 가스트린에 의해 역전될 수 있습니다.

프로토콜 (참조)

세포 분석:

[4]
  • 세포주

    HCT116, SW480, HEK293W cells

  • 농도

    2.5, 5.0, 10 μM

  • 배양 시간

    24 h

  • 방법

    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.
동물 연구:

[5]
  • 동물 모델

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

  • 용량

    4 mg/kg/day

  • 투여

    --

참조

  • 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/

고객 제품 검증

<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.

데이터 출처 [ , , 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.

데이터 출처 [ , , J Neuroimmunol, 2017, 305:154-161 ]

Sellecks (-)-Parthenolide 인용됨 27 출판물

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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