ChemicalBook > CAS DataBase List > FM-381

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

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FM-381 Property

storage temp.: 2-8°C
solubility: DMSO: 2mg/mL, clear (warmed)
form: powder
color: white to beige

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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.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1979
Product name: FM-381
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $150
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1979
Product name: FM-381
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $462
Updated: 2025/07/31

Cayman Chemical

Product number: 23204
Product name: FM-381
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 23204
Product name: FM-381
Purity: ≥98%
Packaging: 5mg
Price: $151
Updated: 2024/03/01

Cayman Chemical

Product number: 23204
Product name: FM-381
Purity: ≥98%
Packaging: 10mg
Price: $278
Updated: 2024/03/01

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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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2226521-65-7, FM-381Related Search:

FM479 N-(3-TRIETHYLAMMONIUMPROPYL)-4-(4-(DIBUTYLAMINO)STYRYL)PYRIDINIUM DIBROMIDE ESTETROL Ethylamine (-)-Varitriol

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

FM-381, 10 mM in DMSO

2226521-65-7