1334493-07-0

BP-1-102 is a potent and selective STAT3 inhibitor. STAT3 is a cytoplasmic transcription factor that induces the expression of genes related to tumorigenesis. BP 1-102 exhibits antitumor activity against Waldenstrom macroglobulinemia, a rare form of B cell non-Hodgkin lymphoma.

Primary Target
Stat3

General method: Benzyl-protected salicylic acid (1 eq.) was dissolved in a stirred solvent mixture of methanol/tetrahydrofuran (1:1, v/v, 0.1 M). After thorough degassing, 10% palladium/carbon catalyst (10 mg/mmol) was cautiously added. The solution was bubbled with hydrogen gas for 5 minutes, followed by continuous stirring of the reaction under hydrogen atmosphere for 3 hours. Upon completion of the reaction, the hydrogen was removed, the palladium catalyst was removed by filtration, and the filtrate was concentrated under reduced pressure.

STAT3: 6.8 μM (IC₅₀)

[1] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 18, p. 5605 - 5609
[2] ACS Medicinal Chemistry Letters, 2013, vol. 4, # 11, p. 1102 - 1107
[3] Journal of Medicinal Chemistry, 2013, vol. 56, # 18, p. 7190 - 7200