Harringtonolide 是一种有效的RACK1抑制剂,在 A375 细胞中IC50=39.66 μM。Harringtonolide 通过影响FAK和RACK1的相互作用来抑制上皮-间充质转化 (EMT) 过程和细胞增殖。Harringtonolide 具有抑制植物生长、抗病毒、抗炎、抗增殖活性。
生物活性 | Harringtonolide is a potentRACK1inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction betweenFAKandRACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities[1]. |
IC50& Target | IC50: 39.66 μM (RACK1) in A375 cells[1] |
体外研究 (In Vitro) | Harringtonolide (0-50 μM; 24 hours) exhibits good antiproliferation activity in A375 cells with IC50of 39.66 μM[1]. Harringtonolide (0-20 μM; 1 hour) restrains the proteolysis of RACK1 by Pronase, and protects temperature-dependent degradation of RACK1[1]. Harringtonolide (0-4 μM; 24 hours) suppresses the phosphorylation of FAK dose-dependently and inhibits Src and STAT3, the downstream proteins of FAK[1]. Harringtonolide (0-4 μM; 24 hours) dose-dependently inhibits the RACK1–FAK interaction in A375 cells[1].
Cell Proliferation Assay Cell Line: | A375 melanoma cells[1] | Concentration: | 0-50 μM | Incubation Time: | 24 hours | Result: | Showed good antiproliferation activity with IC50of 39.66 μM. |
Western Blot Analysis Cell Line: | A375 melanoma cells[1] | Concentration: | 0, 0.5, 1, 2, 4 μM | Incubation Time: | 24 hours | Result: | Suppressed the phosphorylation of FAK dose-dependently and inhibited Src and STAT3, the downstream proteins of FAK. |
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结构分类 | - Ketones, Aldehydes, Acids
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来源 | - Plants
- Cephalotaxaceae
- harringtonia
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |