BP-1-102

BP-1-102 是有口服活性的转录因子 Stat3 的小分子抑制剂，其 IC₅₀ 值为 6.8 μM。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