Sigma-Aldrich Stat3 Inhibitor Xx, Ins3-5

Assay

≥98% (HPLC)

Quality Level

100

Form

powder

Potency

13.8 μM IC₅₀

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

orange

Solubility

DMSO: 50 mg/mL

Storage Temp.

2-8°C

Smiles String

O=C1/C(C=C(C2=CC=CC=C2)N1C3=CC=C(C=C3)C(O)=O)=C/C4=CC=C(C=C4)[N+]([O-])=O

General Description

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.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.

Biochem/Physiol Actions

Cell permeable: yesPrimary 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

Huang, W., et al. 2014.ACS Chem. Bio. 9,1188.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany