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CAS No. : 213261-59-7
MCE 国际站:RITA
产品活性:RITA 是一种有效的 p53-HDM-2 相互作用抑制剂,可与 p53dN 结合,Kd 值为 1.5 nM,同时能够诱导 DNA-DNA 交联。
研究领域:Apoptosis | Autophagy | Cell Cycle/DNA Damage
作用靶点:MDM-2/p53 | Autophagy | DNA Alkylator/Crosslinker
In Vitro: RITA inhibits p53-HDM-2 interaction, binding to p53dN, with a Kd of 1.5 nM. RITA (10 μM) blocks complex formation between p53 and HDM-2 in HCT116 cells and HDFs and in NHF-ERMyc cells irrespective of c-Myc expression. RITA (0.5 μM) reduces the viability of tumor cells in a wild-type p53-dependent manner. Moreover, RITA (0.1 μM) induces p53-dependent apoptosis. RITA induces p53 but does not via DNA damage-signaling pathway. RITA (NSC 652287) induces DNA-DNA cross-links. RITA induces G2-M cell cycle arrest at 10 nM and causes apoptosis at 100 nM. RITA (100 nM) also elevates p53 and causes dose-dependent effects on p21WAF1 protein levels. RITA inhibits the growth of HeLa and CaSki cells, with IC50s of 1 and 10 μM. In addition, RITA (1 μM) stabilizes p53 by inhibiting p53/E6AP interaction.
In Vivo: RITA (0.1, 1 or 10 mg/kg, i.p.) shows potent antitumor activity in SCID mice bearing HCT116 and HCT116 TP53 / xenografts. RITA (10 mg/kg, i.p.) also suppresses the growth of HeLa cells in SCID mice.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Ferroptosis Compound Library | Pyroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Transcription Factor-Targeted Library | Anti-Colorectal Cancer Compound Library | Protein-protein Interaction Inhibitor Library | Busulfan | Carboplatin-d4 | p53 (17-26) | p53 and MDM2 proteins-interaction-inhibitor (racemic) | Navtemadlin | (+)-CBI-CDPI1 | 2-Iodoacetamide | Duocarmycin GA | Antitumor agent-60 | Palifosfamide tromethamine | Mipicoledine | OBI-3424 | Lurbinectedin-d3 | Roslin 2 bromide | Amifostine trihydrate | MX69 | ADH-6 TFA | Duocarmycin DM free base | Carmustine | RG7112 | SCH529074 | CBL0137 hydrochloride | MA242 | MD-224 | MB710 | NSC59984 | MDM2/4-p53-IN-1 | Oxychlororaphine | Illudin S
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Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-13424
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