Cat.No. | Name | Information |
---|---|---|
M2943 | Pifithrin-μ | Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy. |
M2036 | Pifithrin-α | Pifithrin-α is an inactivator of p53 that blocks p53-dependent transcriptional activation and apoptosis. |
M2578 | RITA | RITA (NSC 652287) is a MDM2 inhibitor and DNA damage agent for A498 (wild type) and TK-10 (mutation) cell lines with a GI50 of 17 nM and 32 nM, respectively. |
M43013 | Rezatapopt | Rezatapopt is a first-in-class p53 reactivator that selectively binds to the mutated p53 Y220C protein and restores wild-type activity, used to inhibit solid tumor with p53 mutation. |
M41719 | MS78 | MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. |
M41357 | SLMP53-2 | SLMP53-2 is a mutant p53 reactivator. |
M41353 | p53 CBS | p53 CBS (p53 Consensus binding sequence) is a biological active peptide. |
M31002 | ADH-6 TFA | ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases. |
M30033 | p-nitro-Pifithrin-α | p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet . non-alcoholic fatty liver disease. |
M29665 | C16-Ceramide | C16-Ceramide is a natural small molecule activating p53 through the direct and selective binding. |
M29381 | ADH-6 | ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases. |
M28916 | BI-0252 | BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis. |
M28415 | AM-8735 | AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM. |
M28375 | RO-5963 | RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively. |
M28358 | MI-1061 TFA | MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity. |
M28357 | MI-1061 | MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity. |
M28282 | Exaluren | Exaluren (ELX-02) is an synthetic eukaryotic ribosome-selective glycoside that induces read through of nonsense mutations, resulting in normally localized full-length functional proteins. Exaluren is used for the research of cystic fibrosis caused by nonsense mutations. |
M28049 | SP-141 | SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells. |
M20697 | Triglycidyl Isocyanurate (Teroxirone) | Triglycidyl Isocyanurate, also known as Teroxirone, is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry. |
M19138 | Sanggenol L | Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells. Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p |
M13552 | CTX1 | CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system. |
M13550 | Amifostine thiol | Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine . Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway. |
M11440 | PC14586 | PC14586 is the first-in-class oral small molecule p53 Y220C activator to enter the clinical phase, which induces the transformation of p53 protein from mutant to wild-type conformation in a dose-dependent manner. |
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