BP-1-102 is an orally bioavailable, small-molecule inhibitor of STAT3 with Kd of 504 nM.
BP-1-102 blocks Stat3-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 suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and KLF8, blocks Stat3-NF-κB cross-talk, and enhances E-cadherin expression.
BP-1-102 inhibits growth of human breast and lung tumor xenografts.
