BP-1-102

STAT

-20

BP-1-102 is an orally active, effective, and specific STAT3 inhibitor that binds Stat3 (Kd: 504 nM), blocks Stat3-phosphotyrosine (pTyr) peptide interactions and Stat3 activation (4-6.8 μM), and selectively inhibits the migration, survival, growth, and invasion of Stat3-dependent tumor cells. The BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of [c-Myc, Bcl-xL, Cyclin D1, Survivin, and VEGF].

BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor. BP-1-102 binds Stat3 with an affinity (K(D)) of 504 nM, blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 uM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8, which is identified as a Stat3 target gene that promotes Stat3-mediated breast tumor cell migration and invasion.