FM-381
FM-381 Basic information
- 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
- 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-381Supplier
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 021-61350663 13052117465
- sales@zehanbiopharma.com
- Tel
- 027-65388397 18164111589
- 3321478047@qq.com
- Tel
- 17754423994 17754423994
- 2853530910@QQ.com
- Tel
- 21-31433387 15618786686
- sales@rechemscience.com