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Pifithrin-µ

CAS No. : 64984-31-2

MCE 国际站：Pifithrin-µ

产品活性：Pifithrin-µ 是一种 p53 和 HSP70 的抑制剂，具有抗肿瘤和神经保护作用。

研究领域：Apoptosis | Metabolic Enzyme/Protease | Cell Cycle/DNA Damage | Autophagy

作用靶点：MDM-2/p53 | HSP | Autophagy

In Vitro: Pifithrin-µ (10 µM) is a p53 inhibitor, which inhibits p53 binding to mitochondria by reducing its affinity to antiapoptotic proteins Bcl-xL and Bcl-2 but has no effect on p53-dependent transactivation, activity of caspases 2, 8, 9 and 10 in a cell-free system, or NF-κB-dependent transcription. Pifithrin-µ (PES) time- and dose-dependently reduces viability in A549 cells, with IC₅₀s of 44.9 and 25.7 µM at 24 h and 48 h. Pifithrin-µ (20 µM) suppresses the cell migration, induces cell cycle arrest and cell apoptosis in A549 and H460 cells. Pifithrin-µ (10 or 20 µM) inhibits activities of AKT, ERK, and Hsp70 in A549 and H460 cells. Pifithrin-µ (20 µM) sensitizes A549 and H460 cell lines to TRAIL-induced cell proliferation inhibition and apoptosis.

In Vivo: Pifithrin-µ (40 mg/kg, i.p.) shows no protective effect against doses of radiation that cause gastrointestinal syndrome in mice. Pifithrin-µ (PES, 10 mg/kg) shows antitumor effect in mice bearing A549 cells. Pifithrin-µ exhibits neuroprotective effect with the P53-inhibitor pifithrin-µ after cardiac arrest in a rodent model.

相关产品：Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Ferroptosis Compound Library | Pyroptosis Compound Library | Cytoskeleton Compound Library | Glutamine Metabolism Compound Library | Neuroprotective Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Tamoxifen | Tanespimycin | Nutlin-3a | Pifithrin-α hydrobromide | Geldanamycin | Palmitic acid | Eprenetapopt | Rocaglamide | VER-155008 | Arimoclomol maleate | Amifostine | PU-WS13 | RITA | MKT-077 | KNK437 | KRIBB11 | MI⁻⁷73 | Paeoniflorin | Pifithrin-α, p-Nitro, Cyclic | Retaspimycin Hydrochloride | TRC051384 | ML346 | NSC319726 | Radicicol | Amifostine thiol dihydrochloride | Teprenone

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