Cayman BMH-21

BMH-21 is an inhibitor of RNA polymerase I. It binds to GC-rich sequences in DNA and ribosomal DNA (rDNA) and inhibits RNA polymerase I transcription in vitro. It inhibits expression of the 47S rRNA transcript (IC₅₀ = 60 nM), disrupts the structure of the nucleolus, and leads to removal of the RNA polymerase complex from rDNA by inducing dissociation and destruction of RPA194 through a proteasome-dependent mechanism. BMH-21 also activates p53 in the nanomolar range. It reduces viability of several cancer cell lines but not of non-cancerous cells (IC₅₀s = 0.7, 1.9, ≥40, and 2.7 µM for A375, human diploid fibroblasts, primary human melanocytes, and HIMEC cells, respectively). BMH-21 intercalates with DNA but does not induce DNA damage via the ataxia-telangiectasia mutated (ATM) kinase pathway. BMH-21 (25 mg/kg) inhibits tumor growth in melanoma and colon cancer mouse xenograft models.

WARNING This product is not for human or veterinary use.