(R,R)-VVD-118313 is the isomer of VVD-118313 (Showed labeling of recombinant WT-JAK1 and C810A-JAK1, but not C817A-JAK1.
Inhibited WT- and C810A-JAK1 phosphorylation with even greater potency than STAT1/STAT3 phosphorylation.
VVD-118313 (化合物 5a;25-50 mg/kg;皮下注射;单剂量) 抑制 TYK2 敲除小鼠中的 JAK1 信号传导[1]。
[1]. Kavanagh ME, et, al. Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine. Nat Chem Biol. 2022 Sep 12.
















