irak1

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).

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.

IRAK1/4/pan-FLT3 Kinase-IN-2 (compound 27) is a potent dual inhibitor of IRAK1/4 and FLT3 with IC50 values of 10 nM, 0.7 nM, and < 0.5 nM, respectively. This compound enhances survival in mice models of acute myeloid leukemia.

IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor. It suppresses IL-6 release in murine J774A cells and human THP-1 cells, with IC50 values of 4.57 μM and 6.51 μM, respectively. Additionally, IRAK1-IN-1 alleviates LPS-induced acute lung injury and DSS-induced colitis in mice.

Anthraquinone-2-carboxylic acid acts as a potent anti-inflammatory and antinociceptive component in vivo, thus contributing to the immune regulatory role of fruits and herbs.

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

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

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

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.

TAK-756 is a TAK1 inhibitor that selectively targets IRAK1/4 and exhibits excellent intra-articular pharmacokinetic properties. TAK1 is a potential molecular target for osteoarthritis (OA) due to its complementary anti-catabolic and anti-inflammatory effects.

IRAK4 modulator-2 (Compound 5) is a selective dual inhibitor of IRAK4 and IRAK1, with IC₅₀ values of 0.005 μM and 0.97 μM respectively. It may be employed in research concerning autoimmune and inflammatory diseases such as rheumatoid arthritis, psoriasis, and inflammatory bowel disease.

AF-45 inhibits IRAK4 and IRAK1 with IC50 values of 128 nM and 1765 nM, respectively. It suppresses the release of IL-6 and TNF-α in macrophages, with IC50 ranges of 0.53-1.54 μM and 0.6-2.75 μM, respectively. Additionally, AF-45 acts as an inhibitor of the NF-κB/MAPK signaling pathway. In mouse models, AF-45 exhibits anti-inflammatory activity against DSS-induced ulcerative colitis and lipopolysaccharide-induced acute lung injury. In rat models, AF-45 demonstrates favorable pharmacokinetic properties.

NCGC1481 is a potent inhibitor of FLT3 and IRAK1/4 with improved stability, solubility, and permeability properties.

JH-X-119-01 hydrochloride is a potent, selective inhibitor of interleukin-1 receptor-associated kinase 1 (IRAK1) that effectively alleviates lipopolysaccharide (LPS)-induced sepsis in mice.

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).

JH-I-25 is an IRAK1 kinase inhibitor.

Larotinib mesylate hydrate is a potent, broad-spectrum, and orally active tyrosine kinase inhibitor (TKI), primarily targeting EGFR with an IC50 value of 0.6 nM.

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

JNJ-1013 is a potent and selective IRAK1 degrader, with IC50 values of 72 nM for IRAK1, 443 nM for IRAK4, and 1071 nM for VHL FP. It induces apoptosis, increases cleaved PARP expression, and decreases the expression of IRAK1, p-IKBα, and pSTAT3(Tyr705) [1].

KME-2780 is a potent, selective dual inhibitor of IRAK1 and IRAK4, suitable for research on dysregulation in innate immune signaling and hematologic malignancies [1].

Euscaphic acid has anti-diabetic, and anti-inflammatory activities, it inhibits LPS-induced inflammatory responses by interference with the clustering of TRAF6 with IRAK1 and TAK1, resulting in blocking the activation of IKK and MAPKs signal transduction