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CBFß-Runx1 inhibitor II; 7-chloro-5-(2-pyrryl)-3H-1,4-benzo-diazepin-2-(H)-one
Ro 5-3335 is described to kill human leukemia cell lines with CBF fusion proteins. The IC50 value - 1.1 µM. Ro 5-3335 is a benzodiazepine compound. Originally Ro 5-3335 was shown to inhibit gene expression controlled by the human immunodeficiency virus-1 (HIV-1) LTR promoter. The inhibition was specific for the viral transcriptional transactivator Tat. The compound did not inhibit the basal activity of the HIV-1 LTR or the activity of promoters not responsive to Tat. In addition Ro 5-3335 was able to interact with RUNX1 and CBFß directly, repress RUNX1/CBFB-dependent transactivation in reporter assays, and repress runx1-dependent hematopoiesis in zebrafish embryos. Ro5-3335 preferentially killed human CBF leukemia cell lines, rescued preleukemic phenotype in a RUNX1-ETO transgenic zebrafish, and reduced leukemia burden in a mouse CBFB-MYH11 leukemia model. Potential mode of action/Key words: CBF inhibitor
Cfm Oskar Tropitzsch GmbH supplies unique molecules - in this case the cytotoxins for antibodies. These payloads are ultra-toxic drugs, i.e. cytotoxic and/or cytostatic molecules, effective at a low dosage and ...