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RITA

CAS No. : 213261-59-7

MCE 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，K_d 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 K_d 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 p^21WAF1 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：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Ferroptosis Compound Library  |  Pyroptosis Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Cisplatin  |  Oxaliplatin  |  Temozolomide  |  Mitomycin C  |  Carboplatin  |  Cyclophosphamide  |  Streptozocin  |  Nutlin-3a  |  Pifithrin-α hydrobromide  |  Eprenetapopt  |  N-Nitroso-N-methylurea  |  Busulfan  |  Calicheamicin  |  Ifosfamide  |  Amifostine  |  Melphalan  |  Bendamustine hydrochloride  |  Pifithrin-μ  |  MI-773  |  Carmustine  |  Pifithrin-α, p-Nitro, Cyclic  |  Lomustine  |  Thio-TEPA  |  Altretamine  |  NSC319726  |  4-Hydroperoxy cyclophosphamide

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