RMB:580.00/20mg
小白菊内酯
Product name:Parthenolide
CAS：20554-84-1
Molecular Formula:C15H20O3
Molecular Weight:248.32
Biological Activity:
?Parthenolide (PTL) is a sesquiterpene lactone which can induce apoptosis in cancer cells and eradicate cancer stem cells. Parthenolide can deplete HDAC1 protein without affecting other class I/II HDACs.
IC50 value:
Target: HDAC1; Apoptosis inducer; NF-kB
in vitro: Parthenolide (PTL) induces apoptosis and cell cycle arrest in human lung cancer cells. Moreover, PTL treatment in NSCLC cells increases expression of TNFRSF10B/DR5 and PMAIP1/NOXA [1]. parthenolide dose-dependently inhibited RANKL-mediated osteoclast differentiation in BMMs without any evidence of cytotoxicity and the phosphorylation of p38, ERK, and IκB as well as IκB degradation by RANKL treatment. Parthenolide suppressed the expression of NFATc1, OSCAR, TRAP, DC-STAMP, and cathepsin K in RANKL-treated BMMs. Furthermore, parthenolide down regulated the stability of c-Fos protein, but could not suppress the expression of c-Fos [2]. the sesquiterpene lactone parthenolide (PN), which specifically depletes HDAC1 protein without affecting other class I/II HDACs. HDAC1 depletion occurred through proteasomal degradation and resulted in transcriptional consequences comparable to those observed with pan-HDACi [5].
in vivo: The effects of parthenolide (PTN), a nuclear factor-kappa B inhibitor and sesquiterpene lactone, on polyethylene particle-induced osteolysis in vivo were investigated using a mouse calvarial model [3].dimethylamino-parthenolide (DMAPT), a water soluble parthenolide analog, intranasal instillation of low doses of DMAPT significantly reduced the overall lung tumor multiplicity by 39%. Interestingly, the drug was specifically effective (62% reduction) against bigger lung tumors (> 2 mm), which have a higher potential to develop into lung adenocarcinoma in mice [4].
References on Parthenolide：
[1]. Zhao X, et al. Parthenolide induces apoptosis via TNFRSF10B and PMAIP1 pathways in human lung cancer cells. J Exp Clin Cancer Res. 2014 Jan 6;33(1):3.
[2]. Kim JY, et al. Parthenolide inhibits osteoclast differentiation and bone resorbing activity by down-regulation of NFATc1 induction and c-Fos stability during RANKL-mediated osteoclastogenesis. BMB Rep. 2013 Dec 7. pii: 2508.
[3]. Li Y, et al. Parthenolide inhibits polyethylene particle-induced mouse calvarial osteolysis in vivo. J Surg Res. 2013 Oct 19. pii: S0022-4804(13)00973-6.
[4]. Song JM, et al. Dimethylaminoparthenolide (DMAPT), A Water Soluble Parthenolide, Suppresses Lung Tumorigenesis in Vitro and in Vivo and Downregulates the STAT3 Signaling Pathway. Curr Cancer Drug Targets. 2013 Nov 4.
[5]. Gopal YN, et al. Parthenolide specifically depletes histone deacetylase 1 protein and induces cell death through ataxia telangiectasia mutated. Chem Biol. 2007 Jul;14(7):813-23.
(产品仅适用于科学实验,不得用于其他▂目的).
