irak4

IRAK4-IN-4 (compound 15) inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor, has an IC50 of 2.8 nM.

PROTAC IRAK4 degrader-4 (US20190192668A1, compound I-127) is a Cereblon-based PROTAC specifically designed to target and degrade interleukin-1 receptor-associated kinase 4 (IRAK4).

IRAK4-IN-20 is a potent and orally active IRAK4 inhibitor (IC50:3.55 nM). IRAK4-IN-20, which has anti-inflammatory, antitumor and anticancer effects, is often used to treat acute respiratory distress syndrome (ARDS).

IRAK4-IN-8 (VI-177) is an IRAK4 inhibitor used to study diseases related to cancer and inflammation.

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.

IRAK4-IN-7 (CA-4948) is a selective and potent IRAK4 kinase inhibitor with in vivo activity in a TLR4-induced cytokine release model.

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

IRAK4-IN-24 (compound 16), a potent IRAK4 inhibitor, exhibits high clearance (Cl) and low oral bioavailability. It is utilized in research pertaining to inflammatory and autoimmune disorders.

IRAK4-IN-21 is a selective, orally active, potent IRAK4 inhibitor that acts on IRAK4 (IC50: 5 nM) and TAK1 (IC50: 56 nM). IRAK4-IN-21 exhibits potent inhibition of IL-23 production with an IC50 value of 0.17 μM. can be used to study autoimmune diseases, such as plaque psoriasis and psoriatic arthritis.

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-25 (compound 38), a potent oral IRAK4 inhibitor (IC50 = 7.3 nM) with low clearance (Cl = 12 mL/min/kg), effectively suppresses pro-inflammatory cytokine production and demonstrates favorable in vitro safety and ADME profiles. It is suitable for research on inflammatory and autoimmune disorders [1].

PROTAC IRAK4 degrader-1 is a PROTAC (proteolysis-targeting chimera) compound that targets and degrades interleukin-1 receptor-associated kinase 4 (IRAK4).

IRAK4-IN-22 is a selective, orally active, potent IRAK4 inhibitor that acts on IRAK4 (IC50: 3 nM) and TAK1 (IC50: 17 nM). IRAK4-IN-21 exhibits potent inhibition of IL-23 production with an IC50 value of 0.10 μM. IRAK4-IN-21 can be used to study autoimmune diseases, such as plaque psoriasis and psoriatic arthritis.

PROTAC IRAK4 degrader-6 is a potent Cereblon-based compound designed to degrade [interleukin-1 receptor-associated kinase 4 (IRAK4)].

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].

PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau (VHL).

IRAK4-IN-26 (Compound 21), an IRAK4 inhibitor with an IC50 of 6.2 nM, exhibits an oral bioavailability of 21%. It is utilized for the study of inflammatory and autoimmune disorders [1].

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-6 is a selective and orally efficacious inhibitor of IRAK4, demonstrating an IC50 value of 4 nM. This compound specifically targets MyD88 L265P mutant diffuse large B-cell lymphoma [1].

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

PROTAC IRAK4 Degrader-8 (Compound 2) is a PROTAC designed to target IRAK4 with an IC50 of 15.5 nM [1].

PROTAC IRAK4 ligand-1 is a synthetic ligand targeting interleukin-1 receptor-associated kinase 4 (IRAK4).

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-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.

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-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.

PROTAC IRAK4 Ligand-3 serves as a ligand for PROTAC IRAK4 Degrader-7 and is utilized in cancer research [1].

IRAK4-IN-9 (compound 73) is a highly potent IRAK4 inhibitor with an IC50 value of 1.5 nM, effectively blocking MyD88-dependent signaling and showing significant potential for researching inflammatory diseases, autoimmune diseases, and cancer [1].

IRAK4-IN-28 (compound 42), an orally-active IRAK4 inhibitor (IC50=8.9 nM), exhibits strong binding affinity with a Kd of 0.58 nM for the target enzyme. It is utilized for research purposes in the study of inflammation and autoimmune diseases [1].

IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor with an IC50 of 8.7 nM. It effectively suppresses cell growth and induces apoptosis in the MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell line, making it a valuable agent for DLBCL research [1].

PROTAC IRAK4 degrader-5 is a Cereblon-based compound designed to selectively degrade IRAK4.

PROTAC IRAK4 Degrader-2 (Compound 9) is a PROTAC-based degrader that potently reduces IRAK4 levels, achieving a DC50 of 151 nM in peripheral blood mononuclear cells (PBMCs). It also notably decreases IRAK4 protein levels with a DC50 of 36 nM in the same cell type and inhibits several cytokines in PBMCs [1].

PROTAC IRAK4 degrader-7 (Compound I-417) is an orally administered agent with antitumor properties, functioning as a PROTAC IRAK4 degrader [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.

IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4.

IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 receptor-associated kinase-4 (IC50 = 4 μM).

IRAK inhibitor 4 is a compound that functions as an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It specifically targets and inhibits the activity of IRAK4. The (trans) form of IRAK inhibitor 4 refers to its specific molecular configuration.

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

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

Thalidomide 4-fluoride (E3 ligase Ligand 4) (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand. Thalidomide 4-fluoride can be used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis.

Zabedosertib (BAY 1834845) is an inhibitor of IRAK4 with immunomodulatory potential. Zabedosertib protects against acute respiratory distress syndrome, a new study suggests.

HS271 is a selective, highly potent and orally active IRAK4 inhibitor (IC50= 7.2 μM). HS271 shows excellent enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK-1 (Interleukin-1 Receptor-Associated Kinase 1).

IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor-associated kinase 4 [IRAK-4, IC50: 160 nM].

HPK1-IN-7 is an orally active HPK1 inhibitor. It shows selectivity against IRAK4 (59 nM) and GLK (140 nM).

IRAK inhibitor 1 is an effective IRAK-4 inhibitor (IC50: 216 nM), is poorly active against JNK-1 (IC50: 3.801 μM) and JNK-2 (IC50>10 μM).

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].