IRAK Inhibitor

IRAK4-IN-31 (Compound II) is a crystalline IRAK4 inhibitor. IRAK4-IN-31 can be used in myelodysplastic syndrome (MDS) research.

IRAK4-IN-33 (Compound 22) is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC₅₀ 0.36 nM. IRAK4-IN-33 can block the pro-inflammatory signaling pathway mediated by IRAK4 and inhibit the release of TNFα and IFNα. IRAK4-IN-33 shows weak inhibition for hERG channel (IC₅₀ > 30 μM). IRAK4-IN-33 can be used for the research of inflammation and immunology, such as rheumatoid arthritis.

BI1543673 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. BI1543673 can reduce the inflammatory response stimulated by TLR4 and TLR7/8 in human lung tissue. BI1543673 can decrease inflammatory signaling in a mouse model of lung inflammation induced by LPS.

AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).

DW18134 is an inhibitor for interleukin receptor-associated kinase 4 (IRAK 4) with an IC₅₀ of 11.2 nM. DW18134 inhibits phosphorylation of IRAK4 and IKK, downregulates the secretion of TNF-α and IL-6. DW18134 attenuates the Lipopolysaccharides (HY-D1056)-induced peritonitis and DSS-induced colitis in mouse models, and protects the intestinal barrier function .

AF-45 inhibits IRAK4 and IRAK1, with IC₅₀s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC₅₀s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models.

BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC₅₀ of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7.

IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor. IRAK1-IN-1 inhibits the release of IL-6 with the IC₅₀ values of 4.57 μM and 6.51 μM on mouse cells J774A. 1 and human cells THP-1, respectively. IRAK1-IN-1 alleviats LPS (HY-D1056)-induced acute lung injury (ALI) and DSS(HY-116282C)-induced colitis in mice.

BMS-986126 is a potent, selective, and orally active IRAK4 inhibitor (IC₅₀ = 5.3 nM). BMS-986126 broadly inhibits MyD88-dependent signaling pathways. BMS-986126 demonstrates robust activity in the MRL/lpr and NZB/NZW murine models of lupus, inhibiting multiple pathogenic responses. BMS-986126 can be used for autoimmune diseases research, such as lupus erythematosus (SLE).

KTX-955 is an antumor and effective IRAK4 degrader, with DC₅₀ values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively.

IRAK4-IN-35 is an orally active IRAK4 inhibitor with an IRAK4 IC₅₀ of 9.88 nM. IRAK4-IN-35 also inhibits JAK3, EGFR, CDK2 with IC₅₀ values of 6.72 nM, 32.35 nM, and 39.08 nM, respectively. IRAK4-IN-35 inhibits the production of proinflammatory cytokines, blocks inflammatory signaling pathways, and reduces serum TNF-α levels and spleen index in mouse models of acute inflammation. IRAK4-IN-35 decreases the disease activity index, paw swelling degree, and spleen index in a collagen-induced arthritis mouse model. IRAK4-IN-35 can be used for the research of rheumatoid arthritis.

IRAK4-IN-28 (compound 42) is an orally active IRAK4 inhibitor (IC₅₀=8.9 nM). IRAK4-IN-28 has binding affinity for IRAK4 with a Kd of 0.58 nM. IRAK4-IN-28 can be used in the research of inflammation and autoimmune diseases.

IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC₅₀ of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .

IRAK4-IN-12 (compound 37) is a potent IRAK4 inhibitor with an IC₅₀ of 0.015 µM. IRAK4-IN-12 shows cell pIRAK4 potencies with an IC₅₀ of 0.5 µM.

IRAK4-IN-30 (Compound I) is the inhibitor for IRAK4 with IC₅₀ of 0.6 nM.

IRAK4-IN-17 (Compound 5) is a potent IRAK4 inhibitor with the IC₅₀ of 1.3 nM. IRAK4-IN-17 can be used in large B-cell lymphoma (DLBCL) research.

IRAK1 Human Pre-designed siRNA Set A contains three designed siRNAs for IRAK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

ND-2158 is a competitive IRAK4 inhibitor, with the K_i of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo.

FLT3/IRAK4-IN-1 is a selective FLT3/IRAK4 inhibitor with the remarkable activity towards FLT3-WT (IC₅₀ = 1.95 nM), FLT3-D835Y (IC₅₀ = 3.22 nM) and IRAK4 (IC₅₀ = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML).

Irak1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Irak1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.