irak4-in-4

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.

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.

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].

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).

BI1543673 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It can diminish inflammatory responses in human lung tissue stimulated by TLR4 and TLR7/8. Additionally, BI1543673 reduces inflammatory signaling in a mouse lung inflammation model induced by LPS.

PROTAC IRAK4 ligand-4, a Ligand for Target Protein for PROTAC (Ligand for Target Protein for PROTAC), exhibits anti-tumor activity and is utilized in synthesizing PROTAC IRAK4 degrader-12. This compound serves as a targeted ligand with specific applications in the development of cancer therapeutics.

IRAK1/4/pan-FLT3 Kinase-IN-1 (Compound 31) is a potent inhibitor of IRAK1, IRAK4, and FLT3 kinases, demonstrating IC50 values of 5 nM for IRAK1, 0.6 nM for IRAK4, and less than 0.5 nM for FLT3. It exhibits favorable pharmacokinetic properties and holds promise for research in acute myeloid leukemia, with survival extension effects comparable to Gilteritinib.

MAPK-IN-4 (Compound c1) is an orally active anti-inflammatory agent that inhibits the expression and release of pro-inflammatory cytokines IL-6 and TNF-α induced by LPS. It interacts with IRAK4 to exert its anti-inflammatory effects by inhibiting the MAPK pathway.

LC-MI-3 is an orally active and potent PROTAC degrader of interleukin-1 receptor-associated kinase 4 (IRAK4), with a DC50 value of 47.3 nM. It effectively inhibits the activation of downstream NF-κB signaling. LC-MI-3 is applicable for research in both acute and chronic inflammatory skin conditions.

IRAK4-IN-32 (Compound 10) is a potent inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), with an enzymatic IC50 value of 18.86 nM and a cellular IC50 value of 6.19 nM. It is promising for research in inflammation and autoimmune disease studies.

IRAK4-IN-33 (Compound 22) is a selective and potent orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) with an IC50 value of 0.36 nM. It effectively blocks pro-inflammatory signaling pathways mediated by IRAK4 and inhibits the release of TNFα and IFNα. Additionally, IRAK4-IN-33 demonstrates weak inhibition of the hERG channel (IC50 value greater than 30 μM). This compound is applicable in inflammation and immunology research, such as studies on rheumatoid arthritis.

IRAK4-IN-34 (compound 19) is a potent, highly selective, orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), with an IC50 of 0.73 nM. It demonstrates excellent selectivity against hERG kinase and other kinases, possesses favorable in vivo pharmacokinetic properties, and is applicable for research in inflammatory diseases.

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

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-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-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.

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].

Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).