KTX-497 is an orally active IRAK4 degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology[1].
ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199.
A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1; inhibited IL-1β- or TLR ligand lipopolysaccharide (LPS)-induced IL-6 production in human lung alveolar epithelial cells, fibroblast-like synoviocytes, and peripheral blood mononuclear cells; significantly reduces urinary protein excretion and preventd the development of glomerulosclerosis and interstitial fibrosis without affecting the blood pressure in mice model of chronic kidney disease.
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[1].
KTX-955 is a potent IRAK4 degrader with DC50 values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively. KTX-955 can be used to research anticancer[1][2].
CA-4948 is a selective and potent IRAK4 inhibitor.
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[1].
Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].
IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM[1].
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[1].
IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].
PROTAC IRAK4 degrader-8 (compound 2) is a PROTAC targeting to IRAK4 (IC50=15.5 nM)[1].
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[1].
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[1].
CA-4948 is a potent, selective and orally bioavailable IRAK4 kinase inhibitor with an IC50 of < 50 nM. CA-4948 can be used for the treatment of lymphoma[1].
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[1].
PROTAC IRAK4 degrader-5 is a PROTAC-based IRAK4 degrader extracted from patent US20190192668A1, compound I-171[1].
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[1].
IRAK4-IN-9 (compound 73) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-9 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer[1].
IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-10 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer[1].
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.
IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
PROTAC IRAK4 degrader-1 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively[1].
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[1][2].
HG-12-6 is a small-molecule inhibitor that bind preferentially to unphosphorylated IRAK4 with IC50 of 165.1 nM, displays 15-fold selectivity over phosphorylated IRAK4 (IC50=2876 nM); binds as type II inhibitor with IRAK4 in a “DFG-out” conformation.
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.
KTX-612 is an orally active IRAK4 degrader with a DC50 value of 7 nM. KTX-612 can be used for the research of oncology[1].
IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.