JH-X-119-01 is a highly potent, selective and covalent inhibitor of IRAK1 with IC50 of 9 nM.
JH-X-119-01 irreversibly and covalently labels IRAK1 at C302.
JH-X-119-01 displays no inhibition of IRAK4 at 10 uM, shows exceptional kinome selectivity as assessed by KinomeScan (468 kinases) at 1 μM with off-target inhibition of only two additional kinases, YSK4 (IC50=57 nM) and MEK3.
JH-X-119-01 exhibits moderate cell killing effects in a panel of WM cells, DLBCL cells, and lymphoma cells expressing MYD88.
