runx1-cbfb

RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their specific targets. This compound triggers p53-dependent apoptosis and suppresses the proliferation of cancer cells. Furthermore, RUNX-IN-1 has demonstrated efficacy in impeding tumor progression in PANC-1 xenograft mice [1].

Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro5-3335 also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.