FM-381
- Product Name
- FM-381
- CAS No.
- 2226521-65-7
- Chemical Name
- FM-381
- Synonyms
- FM-381;CS-2854;FM-381; FM 381; FM381;FM-381, 10 mM in DMSO;inhibit,JAK,FM-381,Inhibitor,Janus kinase,FM 381;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;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-;(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;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)-
- CBNumber
- CB63339879
- Molecular Formula
- C24H24N6O2
- Formula Weight
- 428.49
- MOL File
- 2226521-65-7.mol
FM-381 Property
- storage temp.
- 2-8°C
- solubility
- DMSO: 2mg/mL, clear (warmed)
- form
- powder
- color
- white to beige
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H332Harmful if inhaled
H335May cause respiratory irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P310Immediately call a POISON CENTER or doctor/physician.
N-Bromosuccinimide Price
- Product number
- SML1979
- Product name
- FM-381
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $150
- Updated
- 2025/07/31
- Product number
- SML1979
- Product name
- FM-381
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $462
- Updated
- 2025/07/31
- Product number
- 23204
- Product name
- FM-381
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 23204
- Product name
- FM-381
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $151
- Updated
- 2024/03/01
- Product number
- 23204
- Product name
- FM-381
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $278
- Updated
- 2024/03/01
FM-381 Chemical Properties,Usage,Production
Uses
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
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
IC 50
JAK3: 127 pM (IC50)
References
[1] Forster M, et al. Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. Cell Chem Biol. 2016 Nov 17;23(11):1335-1340. DOI:10.1016/j.chembiol.2016.10.008
FM-381 Preparation Products And Raw materials
Raw materials
Preparation Products
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