General description
A cell-permeable, orally bioavailable amidosalicylic acid compound that selectively binds the three subpockets of Stat3 SH2 domain surface (KD = 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.
Biochem/physiol Actions
Primary Target
Stat3
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Zhang, X., et al. Proc. Natl. Acad. Sci. USA109, 9623.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51433700
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 573132-10MG
- CAS:
- 1334493-07-0
