irak4-in-1

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

FLT3/IRAK4-IN-1 is a selective inhibitor of FLT3 and IRAK4, exhibiting significant activity against FLT3-WT (IC50= 1.95 nM), FLT3-D835Y (IC50= 3.22 nM), and IRAK4 (IC50= 53.72 nM). It demonstrates low cytotoxicity towards normal bone marrow cells, effectively promotes apoptosis, and has potential to overcome resistance. FLT3/IRAK4-IN-1 can be utilized in studies of acute myeloid leukemia (AML).

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-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-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].

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-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.

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.

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-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.

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

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-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.

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.

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.

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.

APH02174 is a highly selective and orally active IRAK4PROTAC degrader, with a DC50 of 4.01 nM in THP-1 cells. It blocks inflammatory signaling by inhibiting IL-6 release and is applicable for researching inflammatory diseases such as psoriasis and rheumatoid arthritis.

PROTACIRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader, demonstrating DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes within PBMCs, respectively. It significantly induces TIR signaling activation and inhibits the expression of circulating pro-inflammatory cytokines in a psoriasis mouse model induced by Imiquimod. PROTACIRAK4 degrader-13 is applicable in the study of neutrophilic inflammatory diseases driven by TLR and IL-1R, such as hidradenitis suppurativa (HS) and atopic dermatitis (AD).

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.