Biochem/physiol Actions

Primary TargetSTAT3

Cell permeable: yes

General description

A cell permeable pyrrolonyl benzoic acid derivative that selectively and non-covalently binds to STAT3 and inhibits its DNA binding activity in a dose and time dependent manner (IC₅₀ = 13.8 µM after 29 hours incubation) and reduces the expression of STAT3 dependent genes (Cyclin D1, survivin, VEGF, MMP-2, MMP-9, and Twist) in A549 and MDA-MB-231 cells. However, it does not affect STAT3 dimerization or binding to the SH2 domain and has no effect on total STAT3 or basal level of Tyr705 phosphorylated STAT3. Preferentially induces apoptosis in cancer cells (A549 and MDA-MB-468) and inhibits their survival, but has much reduced effect on non-cancer IMR90 lung fibroblasts or MCF10A1 mammary epithelial cells. Shown to block cancer cell migration and invasion in a dose- and time-dependent manner.Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell permeable compound that selectively binds to STAT3 and inhibits its DNA binding activity (IC₅₀ = 13.8 µM) and reduces the expression of STAT3 dependent genes.

A cell permeable pyrrolonyl benzoic acid derivative that selectively and non-covalently binds to STAT3 and inhibits its DNA binding activity in a dose and time dependent manner (IC₅₀ = 13.8 µM after 29 hours incubation) and reduces the expression of STAT3 dependent genes (Cyclin D1, survivin, VEGF, MMP-2, MMP-9, and Twist) in A549 and MDA-MB-231 cells. However, it does not affect STAT3 dimerization or binding to the SH2 domain and has no effect on total STAT3 or basal level of Tyr705 phosphorylated STAT3. Preferentially induces apoptosis in cancer cells (A549 and MDA-MB-468) and inhibits their survival, but has much reduced effect on non-cancer IMR90 lung fibroblasts or MCF10A1 mammary epithelial cells. Shown to block cancer cell migration and invasion in a dose- and time-dependent manner.

Legal Information

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

Other Notes

Huang, W., et al. 2014. ACS Chem. Bio.9, 1188.

Packaging

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)