FM381 |
| Katalog-Nr.GC19408 |
FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2226521-65-7
Sample solution is provided at 25 µL, 10mM.
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FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor (IC50 = 127 pM/JAK3, 52 nM/JAK1, 346 nM/JAK2, 459 nM/TYK2 by radiometric assay; [ATP] = 10 μM) that targets JAK3 gatekeeper (GK) Cys909 for a reversible covalent interaction, exhibiting much reduced or little potency against a panel of 409 other kinases. FM-381 is >3-fold more potent than the JAK1/3 inhibitor Tofacitinib (IC50 = 292 pM/JAK3, 496 pM/JAK1, 2.2 nM/JAK2, 8.9 nM/TYK2 by radiometric assay; [ATP] = 10 μM) in blocking JAK1/JAK3-mediated STAT5 phosphorylation in human CD4+ T-cells upon IL-2 stimulation (ECmax ∼100 nM with FM-381), while being ineffective (up to 1 μM) against JAK3-independent STAT1/3 phosphorylation following IL-6 or TNFα stimulation.
Reference
[1].http://www.thesgc.org/chemical-probes/FM-381
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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