BP-1-102

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC₅₀ of 6.8 μM. In Vitro: BP-1-102 binds Stat3 with an affinity K_D of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC₅₀ value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, 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^[1]. In Vivo: Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas^[2]. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth^[1].