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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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STAT3-IN-21, cell-permeable, negative control, a peptide, is a negative control for Stat3 activity detection. |
STAT3-IN-24, cell-permeable
STAT3-IN-24, cell-permeable (PpYLKTK-mts) is a STAT3 peptide inhibitor. |
5-FAM-GpYLPQTV-NH2
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. |
Ac-GpYLPQTV-NH2
Ac-GpYLPQTV-NH2 is a STAT3 inhibitor with an IC50 value of 0.33 μM. |
XZH-5
XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability. |
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