Molecular Formula | C24H24N6O2 |
Molar Mass | 428.486 |
Solubility | DMSO : 12.8 mg/mL (29.87 mM; Need ultrasonic and warming) |
Appearance | Shape powder, color white to beige |
Storage Condition | 2-8°C |
Physical and Chemical Properties | Bioactive FM-381 is a specific inhibitor of JAK3, the inhibition is reversible, covalently bound to JAK3, IC50 is 127 pM. The selectivity for JAK3 is 400 times, 2700 times and 3600 times for JAK1, JAK2 and TYK2 respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.334 ml | 11.669 ml | 23.338 ml |
5 mM | 0.467 ml | 2.334 ml | 4.668 ml |
10 mM | 0.233 ml | 1.167 ml | 2.334 ml |
5 mM | 0.047 ml | 0.233 ml | 0.467 ml |
Target
Target Value
JAK3
(Cell-free) 127 pM
in vitro studies
FM-381 is an effective JAK3 inhibitor, targeting JAK3 Cys909. FM-381 had no activity against BRDs (eg, BRD4, BRPF, CECR, FALZ, TAF1, BRD9). In the concentration-dependent BRET test, the EC50 of the FM-381 was 100 nM. In human CD4 T cells, 100 nM FM-381 can inhibit IL-2-stimulated (JAK3/JAK1)STAT5 phosphorylation; However, even at a concentration of up to 1 μM,FM-381 has no inhibitory effect on (JAK1/2/TYK dependent)STAT3 signal under IL6 stimulation independent of JAK3.