STAT3 Inhibitor XVIII, BP-1-102

A cell-permeable, orally bioavailable amidosalicylic acid compound that selectively binds the three subpockets of Stat3 SH2 domain surface (K_D = 504 nM) and blocks Stat3 phosphorylation, dimerization, and DNA-binding activity in a dose-dependent manner. Preferentially disrupts the high affinity binding between Stat3 and IL-6R/gp130-derived pTyr904 peptide (IC₅₀ = 4.1 µM). Does not exert any significant effect on the phosphorylation status of Shc, Src, JAK1/2, Erk1/2, or Akt. Shown to reduce Stat3-dependent growth, survival, migration, and invasion of tumor cells in vitro and suppress the growth of aberrant Stat3-harboring human breast and lung tumor xenografts (3 mg/kg, i,v. or o.g.) in vivo.

Primary Target
Stat3

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Zhang, X., et al. Proc. Natl. Acad. Sci. USA109, 9623.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany