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Oncrasin-1
Oncogenic Ras Tumor-Inhibiting compound 1, 1-((4-Chlorobenzyl)-1H-indole-3-carboxaldehyde
A cell-permeable indolecarboxaldehyde compound that selectively induces apoptosis in cells harboring mutant K-Ras both in vitro (IC50 = 0.11, 0.25, 1.0, 1.58, and 4.81 µM in H2887, H460, H2122, A549, and T29Kt1 cultures, respectively) and in vivo (75% suppression of H460-derived tumor growth in mice; 100 mg/kg via daily i.p.), while exhibiting little or much reduced potency toward cells with wild-type Ras or mutant N-Ras (IC50 ≥31 µM). Oncrasin-1 treatment is shown to induce PKCι aggregation with splicing factors in the nucleus and dissociation between PKCι and CDK9/Cyclin T1 in K-Ras mutant cultures, resulting in decreased RNA polymerase II phosphorylation and a suppression of RNA processing in general. Oncrasin-1-induced cell death requires the presence of both mutant K-Ras and PKCι, siRNA-mediated knockdown of either enzyme is demonstrated to abolish its cytotoxicity in H460 and T29Kt1 cultures.
产品信息
Form Off-white solid
Molar mass 269.7
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C16H12ClNO
CAS number 75629-57-1
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Irritant |