irak4in1

IRAK4-IN-1 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.

IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor (IC50 = 1.5 nM) that can block the MyD88-dependent signaling pathway and has research potential in inflammatory diseases, autoimmune diseases, and cancer.

FLT3/IRAK4-IN-1 is a selective inhibitor of FLT3 and IRAK4, exhibiting significant activity against FLT3-WT (IC50= 1.95 nM), FLT3-D835Y (IC50= 3.22 nM), and IRAK4 (IC50= 53.72 nM). It demonstrates low cytotoxicity towards normal bone marrow cells, effectively promotes apoptosis, and has potential to overcome resistance. FLT3/IRAK4-IN-1 can be utilized in studies of acute myeloid leukemia (AML).

IRAK4-IN-16 (compound 4) is a potent inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4) with an IC50 of 2.5 nM. It exhibits cytotoxicity against OCI-LY10, TMD8, Ramos, and HT cells, with IC50 values of 0.2, 0.2, 0.6, and 2.7 μM, respectively [1].

IRAK4-IN-11 (compound 6) is a potent IRAK4 inhibitor with an IC50 of 0.008 μM, demonstrating cell pIRAK4 potencies with an IC50 of 0.19 μM [1].

IRAK4-IN-17 (Compound 5) is a highly potent IRAK4 inhibitor with an IC50 value of 1.3 nM [1], and it is particularly valuable for research on large B-cell lymphoma (DLBCL) [1].

IRAK4-IN-13 (compound 21) is a selective and potent IRAK4 inhibitor with an IC50 of 0.6 nM and exhibits high metabolic clearance, possessing an intrinsic human liver microsomal (HLM) clearance of 96 μL/min/mg.

IRAK4-IN-18 is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4) (IC50: 15 nM). It inhibits LPS-induced IL23 production in THP and DC cells and blocks the development of arthritis in rats, making it useful for studying arthritic diseases.

IRAK4-IN-12 (compound 37) is a potent inhibitor of IRAK4 with an IC50 of 0.015 μM and demonstrates cellular pIRAK4 potency with an IC50 of 0.5 μM.

IRAK4-IN-15 is a selective and potent IRAK4 inhibitor (IC50: 0.002 μM) with good human PK prediction and low intrinsic clearance.IRAK4-IN-15 in combination with Acalabrutinib exhibited potent synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL.

IRAK4-IN-14 is a selective, potent, orally active IRAK4 inhibitor (IC50: 0.003 μM) with favorable PK parameters in rats and mice. effect.

IRAK4-IN-19 is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4) with an IC50 of 4.3 nM. It inhibits LPS-induced IL23 production in THP and DC cells and suppresses arthritis development in arthritic model rats. IRAK4-IN-19 can be used to study arthritic diseases.