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Field of application
HS-243 (HS243) is a highly potent, super-selective IRAK-1/4 inhibitor with IC50 of 24/20 nM, respectively.HS-243 shows exquisite potency toward IRAK-1/4 over all other human kinases with only minimal TAK1-inhibiting activity (IC50=0.5 uM).HS-243 binds in the ATP-binding pocket of IRAK-4.HS-243 potently reduces the proinflammatory response of RA cells and macrophages, has distinct cytokine profile from TAK1.HS-243 reduces percentage of survival in pancreatic and breast cancer cell lines.
Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors.
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.
Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research.
THZ-2-118 is a potent selective inhibitor of IRAK1 with IC50 of 14.2 nM;
THZ-2-118 does not inhibitor IRAK4 at 10 uM, also potently inhibits JNK1/2/3 (IC50=1-2 nM).
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