SML1979

FM-381

≥98% (HPLC)

• Synonym(e): (E)-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-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide
• Empirische Formel (Hill-System): C₂₄H₂₄N₆O₂
• CAS-Nummer: 2226521-65-7
• Molekulargewicht: 428.49
• UNSPSC Code: 12352202
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (warmed)
• storage temp.: 2-8°C
• SMILES string: CN(C(/C(C#N)=C/C(O1)=CC=C1C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5)=O)C
• InChI key: GJMZWYLOARVASY-NTCAYCPXSA-N

Beschreibung

Biochem/physiol Actions

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. 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

Highly potent and selective janus kinase JAK3 inhibitor that blocks JAK1/JAK3-mediated STAT5 phosphorylation in human CD4+ T-cells.

Features and Benefits

FM-381 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable