FM-381

FM-381, a chemical probe, 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[1].

Product Specifications

CAS Number

[2226521-65-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H332, H335

Target

JAK

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/FM381.html

Purity

99.58

Solubility

DMSO : 8.33 mg/mL (ultrasonic)

Smiles

CN(C(/C(C#N)=C/C1=CC=C(C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5)O1)=O)C

Molecular Formula

C24H24N6O2

Molecular Weight

428.49

Precautions

H302, H315, H319, H332, H335

References & Citations

[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.