Yuanhuacine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Yuanhuacine (Gnidilatidin)，一种来自 Daphne genkwa 的达芙烷二萜，具有广泛的抗肿瘤活性。Yuanhuacine 是一种具有口服活性的的 DNA 损伤剂。

Yuanhuacine (Gnidilatidin), a diterpene from Daphne genkwa, is an effective and highly selective inhibitor of the basal-like 2 (BL2) subtype of TNBC. Yuanhuacine can induce G2/M cell cycle arrest and has broad anti-tumor activity. Yuanhuacine is an orally active DNA damaging agent.

Yuanhuacine (0.5-1 mg/kg，口服，每日一次，21 天) 抑制小鼠体内肿瘤增殖。Animal Model:H1993 cells implanted xenograft mouse model Dosage:0.5, 1 mg/kg; daily; 21 days Administration:Oral Result:Inhibited tumor growth by 33.4% and 38.8%, respectively, reduced tumor weight, activated AMPK, and inhibited proliferation biomarkers Ki-67 and PCNA in tumor tissues.

Yuanhuacine (0-100 μM，24-72 h) 抑制 H1993，H358，H460，Calu-1，H1299，A549 细胞增殖，IC50 为 0.009，16.5，6.2，4.1，4.0，0.03 μM。Yuanhuacine (0-1000 nM，24 h) 在 H1993 细胞中抑制 p-AMPK 蛋白水平，下调 mTOR 的激活。Yuanhuacine (10-100 nM，0-24 h) 抑制 H1993 细胞迁移。Yuanhuacine (0-16 μM，24 h) 抑制 UMUC3，HCT116 细胞增殖，IC50 为 1.89，14.28 μM。 Yuanhuacine (2 μM，12 h) 诱导 T24T 和 HCT116 细胞 G2/M 期阻滞。Yuanhuacine (0-2 μM，12 h) 通过调节 Sp1 蛋白稳定性，上调 p21 转录和蛋白表达。Cell Viability Assay Cell Line:H1993 cell Concentration:0, 0.00128, 0.0064, 20, 100 μM Incubation Time:24, 48, 72 h Result:Inhibited cell proliferation in a concentration- and time-dependent manner.Western Blot Analysis Cell Line:H1993 cell Concentration:0, 10, 100, 500, 1000 nM Incubation Time:24 h Result:Significantly increased p-AMPK protein levels, decreased ACC levels, inhibited the autophosphorylation of mTOR at Ser2481 site, inhibited Akt, PKC-α, Rac1 and F-actin, and activated the cell adhesion molecule E-cadherin expression.Cell Migration Assay Cell Line:H1993 cell Concentration:10, 100 nM Incubation Time:0, 24 h Result:Inhibited cell migration in a concentration-dependent manner.Cell Viability Assay Cell Line:T24T, UMUC3, HCT116 Concentration:0, 2, 4, 8, 16 μM Incubation Time:24 h Result:Inhibited cell proliferation in a dose-dependent manner.Cell Cycle Analysis Cell Line:T24T, HCT116 Concentration:2 μM Incubation Time:12 h Result:Induced significant G2/M phase arrest.Western Blot Analysis Cell Line:T24T, HCT116 Concentration:0, 1, 2 μM Incubation Time:12 h Result:Up-regulated the expression of p21 protein, but did not show observable induction of p53 protein expression and p53 protein Ser-15 phosphorylation site.

芫花酯甲

Others

Other Targets

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60195-70-2

648.749

C37H44O10

>98% (HPLC)

DMSO : 100 mg/mL (154.14 mM; ultraphonic)

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(-20℃)

With Ice Pack

≥ 2 years