Molecular Formula | C8H5NO4S |
Molar Mass | 211.19 |
Density | 1.621±0.06 g/cm3(Predicted) |
Melting Point | 187-188 °C |
Boling Point | 461.1±45.0 °C(Predicted) |
Solubility | DMSO: >20mg/mL |
Appearance | powder |
Color | white to beige |
Storage Condition | Sealed in dry,2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
In vitro study | Stattic inhibits the binding of gp130 receptor-derived phosphorylated tyrosine-containing peptides to the STAT3 SH2 domain in a strong temperature-dependent manner. Stattic has only a very weak effect on the binding of tyrosine phosphorylated peptides to the SH2 domain of tyrosine kinase Lck. Stattic does not inhibit the dimerization of the other two dimeric transcription factors (c-Myc/Max and Jun/Jun). Stattic inhibits the binding of fluorescein-labeled phosphorylated peptides to the SH2 domains of STAT1 and STAT5b. The concentration of Stattic is 10 μm, which selectively inhibits the binding of DNA to STAT3 dimer. Stattic inhibits phosphorylation of STAT3 at Tyr705, while it has little inhibitory effect on phosphorylation of STAT1 at Tyr701(HepG2 cells) or phosphorylation of JAK1, JAK2, and c-Src(MDA-MB-231 and MDA-MB-235S cells). Stattic increases the rate of apoptosis in a stat3-dependent breast cancer cell line. |
Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. R22 - Harmful if swallowed |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
WGK Germany | 3 |
Hazard Note | Irritant |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.735 ml | 23.675 ml | 47.351 ml |
5 mM | 0.947 ml | 4.735 ml | 9.47 ml |
10 mM | 0.474 ml | 2.368 ml | 4.735 ml |
5 mM | 0.095 ml | 0.474 ml | 0.947 ml |
biological activity | Stattic is the first non-peptide small molecule, which effectively inhibits STAT3 activation and nuclear translocation, the IC50 was 5.1 μm, which was highly selective for stat1. Stattic is the first non-peptide small molecule inhibitor of STAT3, which effectively inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μm, and its selectivity for STAT3 is much higher than stat1. Stattic can induce apoptosis. |
features | Stattic is the first small non-peptide molecule that inhibits the function of the STAT3 SH2 domain, regardless of the STAT3 phosphorylation status in vitro. |
Target | Value |
STAT3 (Cell-free assay) | 5.1 μM |
Use | a potent inhibitor of STAT3 activation and dimerization. Stattic is a small molecule shown to selectively inhibit the activation of the Stat3 transcription factor by blocking phosphorylation and dimerization events. Stattic has been used as a tool for probing the upstream activation of this factor, significantly expressed in many cancer cell lines and interruption of this pathway in breast cancer cell lines lead to an increased apoptotic rate in these cells. Stat3 Inhibitor V, Stattic is an inhibitor of Stat3. |