- FM-381
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- $48.00 / 1mg
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2024-11-19
- CAS:2226521-65-7
- Min. Order:
- Purity: 99.33%
- Supply Ability: 10g
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| Product Name: | FM-381 | | Synonyms: | FM-381;(E/Z)-2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide;FM-381; FM 381; FM381;CS-2854;2-Propenamide, 2-cyano-3-[5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-2-furanyl]-N,N-dimethyl-;2-Propenamide,2-cyano-3-[5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-2-furanyl]-N,N-dimethyl-,(2E)-;2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide;inhibit,JAK,FM-381,Inhibitor,Janus kinase,FM 381 | | CAS: | 2226521-65-7 | | MF: | C24H24N6O2 | | MW: | 428.49 | | EINECS: | | | Product Categories: | | | Mol File: | 2226521-65-7.mol |  |
| | FM-381 Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMSO: 2mg/mL, clear (warmed) | | form | powder | | color | white to beige |
| | FM-381 Usage And Synthesis |
| Biological Activity | 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) th at 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. For characterization details of FM-381, please visit the FM-381 probe summary on the Structural Genomics Consortium (SGC) website.
FM-479 is the negative control for the active probe, FM-381. FM-479 is available from Sigma. To learn more about and purchase FM-479, click here.
To learn about other SGC chemical probes, visit sigma.com/sgc |
| | FM-381 Preparation Products And Raw materials |
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