RDp002 is a potent novel small molecule STAT3 inhibitor, interacts with STAT3 SH2 domain with KD of 4.23 uM, inhibits STAT3 phosphorylation of STAT3 at tyrosine 705 and serine 727 residues.
RDp002 (1 uM) markedly impedes the translocation of p-STAT3 (Tyr705) into the nucleus of MM.1S cells.
RDp002 treatment causes a dose-dependent reduction in IL-6-induced STAT3-dependent luciferase reporter activity in 4 T1 and MDA-MB-468 cells.
RDp002 inhibits the phosphorylation of Tyr705 and Ser727, nuclear translocation, transcriptional activity and the expression of downstream target genes regulated by STAT3.
RDp002 (<10 uM) effectively inhibited the proliferation of TNBC and MM cell lines, including MDA-MB-468, MDA-MB-231, 4T1, U266, RPMI-8226 and MM.1S.
RDp002 induced tumour cell death via the lysosomal pathway.
RDp002 (5-10 mg/kg) suppresses tumour growth in subcutaneous xenograft models of MDA-MB-468.