IRAK Inhibitor

IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC₅₀ of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma.

BIO-7488 is an orally active, selective and blood-brain barrier permeable IRAK4 inhibitor, with an IC₅₀ value of 0.5 nM. BIO-7488 inhibits the production of pro-inflammatory cytokines (IL-1β, TNFα, IL-6) and demonstrates anti-inflammatory effects in both LPS (HY-D1056) and distal hypoxic-middle cerebral artery occlusion (DH-MCAO) ischemic stroke model. BIO-7488 can be used for the study of neuroinflammatory-related diseases, particularly ischemic stroke.

HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC₅₀ values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC₅₀ of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.

IRAK1/4/pan-FLT3 Kinase-IN-1 is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC₅₀s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 can be used for research on AML.

IRAK4-IN-7 is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, extracted from patent WO2015104688 (example 1). IRAK4-IN-7 has the potential for cancer and inflammatory diseases treatment.

Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC₅₀ of 0.6 nM.

IRAK4-IN-20 (Compound BAY-1834845) is an orally active IRAK4 inhibitor with an IC₅₀ of 3.55 nM. IRAK4-IN-20 can be used for acute respiratory distress syndrome (ARDS) research.

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 MYD88^MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.

IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC₅₀ values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC₅₀=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis.

GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC₅₀ values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases.

IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC₅₀ of 4 μM. IRAK-4 protein kinase inhibitor 2 can be used for the research of inflammatory and immune-related conditions or disorders.

IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC₅₀ of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib.

Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC₅₀ of 0.6 nM.

PF-06426779 is a potent and selective inhibitor of interleukin 1 receptor associated kinase 4 (IRAK4), with an IC₅₀ of 0.3 nM.

IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC₅₀ of 216 nM, is poorly active against JNK-1 and JNK-2 with IC₅₀ of 3.801 μM, and >10 μM, respectively.

IRAK inhibitor 2 is an interleukin-1 receptor-associated kinase (IRAK) inhibitor. IRAK inhibitor 2 can be used for the research of inflammatory and immune diseases.

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC₅₀ of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC₅₀s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride can be used for research on AML.

UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.

IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.