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FLLL31 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 (SH2) domain, effective inhibitors of STAT3 phosphorylation. STAT3 plays a critical role in early embryogenesis, but is largely dispensable in normal adult cells and tissues. On the other hand the JAK2/STAT3 signaling pathway is persistently activated in great number of human solid and blood cancers. Such activation is commonly associated with a worse prognosis. FLLL31 is a curcumin derivative locked in diketone-tautomeric form, which supposedly improves binding to SH2 domain. The compound inhibits JAK2 kinase activity and prevents STAT3 phosphorylation. FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.
| Molecular Weight | 424.49 |
| Formula | C25H28O6 |
| CAS Number | 52328-97-9 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related STAT Products |
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| NSC 74859 (S3I-201)
NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM. NSC 74859 (S3I-201) is effective in hepatocellular cancers with disrupted TGF-beta signaling.*The compound is unstable in solutions, freshly prepared is recommended |
| Fludarabine
Fludarabine (NSC 118218) is a STAT1 activation inhibitor and a DNA synthesis inhibitor. Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. Fludarabine markedly inhibited VSMC proliferation in cell culture. Fludarabine also induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Fludarabine exhibits antiproliferative activity (IC50 = 1.54 μM in RPMI cells) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP and survivin expression. |
| Niclosamide
Niclosamide is an inhibitor of STAT3 with an IC50 value of 0.25 μM. |
| Nifuroxazide
Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells. |
| Stattic
Stattic is the first nonpeptidic STAT3 inhibitor, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1. Stattic inhibits STAT3 phosphorylation (at Y705 and S727). |
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