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DEL-22379
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DEL-22379
CAS No. : 181223-80-3
MCE 站:DEL-22379
产品活性:DEL-22379 是一种 ERK 二聚化抑制剂。DEL-22379 易与 ERK2 结合,Kd 为低微摩尔水平,即使在低纳摩尔浓度下也可检测到 EL-22379 与 ERK2 结合。DEL-22379 抑制 ERK2 二聚化,IC50 约为 0.5 μM。
研究领域:MAPK/ERK Pathway | Stem Cell/Wnt | Apoptosis
In Vitro: DEL-22379 is an ERK dimerization inhibitor. DEL-22379 abolishes EGF-induced co-immunoprecipitation of ectopic ERK2 molecules tagged with hemagglutinin (HA) or FLAG epitopes, with an estimated half-maximal inhibitory concentration (IC50) of ~0.5 μM. DEL-22379 inhibits growth of tumor cells harboring RAS-ERK pathway oncogenes. The biological effects of DEL-22379 are investigated on tumor cells in culture. The cytostatic effects of DEL-22379 are compared to those of the MEK inhibitor PD-0325901 and the ERK kinase inhibitor SCH-772984, as reflected by their half-maximal growth inhibitory concentrations (GI50). Cell lines harboring mutant BRAF are the most sensitive to the three compounds. In comparison, wild-type (WT) cell lines for BRAF and RAS are the most resistant, and RAS mutant cells exhibit a range of sensitivities. In cells showing different oncogenic genotypes, distinct sensitivity to DEL-22379 can not be attributed to variations on its effects on dimerization, because DEL-22379 displays similar dimerization- and cytoplasmic signaling-inhibitory dose responses (IC50 of 150-400 nM) regardless of the genotype.
In Vivo: To test DEL-22379 antitumor effects, some of the aforementioned cell lines are xenografted into nude mice, and tumor growth is monitored after intra-peritoneal administration of DEL-22379 at 15 mg/kg. At such a dose, inhibition of ERK dimerization is evident in liver extracts and in xenografted tumors. DEL-22379 markedly inhibits tumor progression for A375 cells (BRAF mutant).
相关产品:Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glutamine Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | PD98059 | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11-7082 | Etoposide | Mitomycin C | CCCP | DAPT | Rote | Etomoxir | Stattic | Docetaxel
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